Reagents and instruments for immunology, cell biology and molecular biology.

Osimertinib [1421373-65-0]

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Cat# HY-15772-100mg

Size : 100mg

Brand : MedChemExpress

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Description

Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC₅₀ of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer^[1].

IC₅₀ & Target^[1]

EGFR^L858R

12 nM (IC₅₀, Enzyme assays)

EGFR^L858R/T790M

1 nM (IC₅₀, Enzyme assays)

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	0.4 μM Compound: AZD9291	Antiproliferative activity against human A431 wild type cells measured after 72 hrs by Sulforhodamine B assay Antiproliferative activity against human A431 wild type cells measured after 72 hrs by Sulforhodamine B assay	[PMID: 31889606]
A-431	GI₅₀	0.596 μM Compound: Osimertinib	Antiproliferative activity against human A-431 cells harboring wild type EGFR measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human A-431 cells harboring wild type EGFR measured after 72 hrs by CellTiter-Glo assay	[PMID: 35486541]
A-431	IC₅₀	0.61 μM Compound: Osimertinib	Antiproliferative activity against human A431 cells harboring WT EGFR after 72 hrs by MTS assay Antiproliferative activity against human A431 cells harboring WT EGFR after 72 hrs by MTS assay	[PMID: 30442506]
A-431	EC₅₀	0.67 μM Compound: Osimertinib	Antiproliferative activity against human A431 cells expressing wild type EGFR incubated for 96 hrs measured on day 5 by CellTiterGlo assay Antiproliferative activity against human A431 cells expressing wild type EGFR incubated for 96 hrs measured on day 5 by CellTiterGlo assay	[PMID: 28853575]
A-431	IC₅₀	0.685 μM Compound: AZD-9291	Antiproliferative activity against human A431 cells harboring wild-type EGFR after 72 hrs by MTT assay Antiproliferative activity against human A431 cells harboring wild-type EGFR after 72 hrs by MTT assay	[PMID: 29534926]
A-431	EC₅₀	0.7 μM Compound: Osimertinib	Antiproliferative activity against human A431 cells harboring wild type EGFR assessed as growth inhibition after 96 hrs by CellTiter-Glo assay Antiproliferative activity against human A431 cells harboring wild type EGFR assessed as growth inhibition after 96 hrs by CellTiter-Glo assay	[PMID: 28603991]
A-431	IC₅₀	0.77 μM Compound: AZD9291	Antiproliferative activity against human A-431 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human A-431 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 32679450]
A-431	IC₅₀	0.77 μM Compound: AZD9291	Cytotoxicity against human A-431 cells assessed as reduction in cell viability measured by MTT assay Cytotoxicity against human A-431 cells assessed as reduction in cell viability measured by MTT assay	[PMID: 34534838]
A-431	IC₅₀	0.821 μM Compound: AZD9291	Antiproliferative activity against human A-431 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human A-431 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 35447433]
A-431	IC₅₀	0.85 μM Compound: Osimertinib	Antiproliferative activity against human A-431 cells harboring EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human A-431 cells harboring EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31951960]
A-431	IC₅₀	0.893 μM Compound: AZD9291	Antiproliferative activity against human A431 cells overexpressing wild-type EGFR after 72 hrs by SRB assay Antiproliferative activity against human A431 cells overexpressing wild-type EGFR after 72 hrs by SRB assay	[PMID: 27131639]
A-431	IC₅₀	0.945 μM Compound: 6; AZD-9291	Antiproliferative activity against human A431 cells harboring wild-type EGFR after 72 hrs by MTT assay Antiproliferative activity against human A431 cells harboring wild-type EGFR after 72 hrs by MTT assay	[PMID: 30471829]
A-431	EC₅₀	0.956 μM Compound: Osimertinib	Antiproliferative activity against human A-431 cells harboring wild type EGFR measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human A-431 cells harboring wild type EGFR measured after 72 hrs by CellTiter-Glo assay	[PMID: 35486541]
A-431	IC₅₀	0.956 μM Compound: 3; AZD9291	Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as inhibition of cell proliferation incubated for 72 hrs by sulforhodamine B colorimetric assay Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as inhibition of cell proliferation incubated for 72 hrs by sulforhodamine B colorimetric assay	[PMID: 28987609]
A-431	IC₅₀	1.19 μM Compound: 4	Antiproliferative activity against human A-431 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human A-431 cells incubated for 72 hrs by MTT assay	[PMID: 31787359]
A-431	IC₅₀	1.226 μM Compound: AZD9291	Cytotoxicity against human A-431 cells harboring wild type EGFR assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay Cytotoxicity against human A-431 cells harboring wild type EGFR assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay	[PMID: 34218082]
A-431	IC₅₀	1.24 μM Compound: AZD9291	Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by resazurin dye based assay Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by resazurin dye based assay	[PMID: 30429956]
A-431	IC₅₀	1.26 μM Compound: 5; AZD9291	Antiproliferative activity against wild type EGFR expressing human A431 cells after 72 hrs by SRB assay Antiproliferative activity against wild type EGFR expressing human A431 cells after 72 hrs by SRB assay	[PMID: 29730192]
A-431	IC₅₀	1.3 μM Compound: 4	Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as inhibition of cell growth by MTT assay Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as inhibition of cell growth by MTT assay	[PMID: 31869655]
A-431	IC₅₀	1.325 μM Compound: 4	Cytotoxicity against human A-431 cells harboring wild type EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human A-431 cells harboring wild type EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 36288657]
A-431	IC₅₀	1.44 μM Compound: 4; AZD9291	Antiproliferative activity human A431 cells incubated for 72 hrs by SRB assay Antiproliferative activity human A431 cells incubated for 72 hrs by SRB assay	[PMID: 31223440]
A-431	IC₅₀	1.51 μM Compound: 6, AZD9291	Antiproliferative activity against human A431 cells overexpressing EGFR assessed as reduction in cell viability by CCK8 assay Antiproliferative activity against human A431 cells overexpressing EGFR assessed as reduction in cell viability by CCK8 assay	[PMID: 32631532]
A-431	IC₅₀	1.604 μM Compound: 3	Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by SRB assay Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by SRB assay	[PMID: 28033579]
A-431	IC₅₀	1310 nM Compound: Osimertinib	Antiproliferative activity against human A-431 cells expressing EGFR wildtype assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human A-431 cells expressing EGFR wildtype assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 35254067]
A-431	IC₅₀	138.7 nM Compound: AZD9291	Antiproliferative activity against human A-431 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay Antiproliferative activity against human A-431 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay	[PMID: 33459024]
A-431	IC₅₀	2.035 nM Compound: 5	Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 35446588]
A-431	GI₅₀	40.1 nM Compound: Osimertinib	Antiproliferative activity against human A431 cells harboring WT EGFR after 72 hrs by MTS assay Antiproliferative activity against human A431 cells harboring WT EGFR after 72 hrs by MTS assay	[PMID: 30442506]
A-431	IC₅₀	5.32 μM Compound: Osimertinib	Antiproliferative activity against human A-431 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human A-431 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 33640672]
A-431	IC₅₀	742 nM Compound: AZD9291	Antiproliferative activity against human A431 cells expressing wild type EGFR assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against human A431 cells expressing wild type EGFR assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 32883633]
A-431	IC₅₀	795.2 nM Compound: AZD9291	Cytotoxicity against human A-431 cells harboring wild-type EGFR measured after 72 hrs by celltiter-glo assay Cytotoxicity against human A-431 cells harboring wild-type EGFR measured after 72 hrs by celltiter-glo assay	[PMID: 33667898]
A-431	EC₅₀	830 nM Compound: 1	Cytotoxicity against human A-431 cells expressing wild type EGFR assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay Cytotoxicity against human A-431 cells expressing wild type EGFR assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay	[PMID: 37197473]
A-431	IC₅₀	84 nM Compound: Osimertinib	Antiproliferative activity against human A431 cells harboring EGFR wild type incubated for 96 hrs by Celltiter-Glo luminescent cell viability assay Antiproliferative activity against human A431 cells harboring EGFR wild type incubated for 96 hrs by Celltiter-Glo luminescent cell viability assay	[PMID: 31689114]
A-431	CC₅₀	967 nM Compound: Osimertinib	Cytotoxicity in human A431 cells assessed as reduction in cell viability incubated for 96 hrs by MTS method Cytotoxicity in human A431 cells assessed as reduction in cell viability incubated for 96 hrs by MTS method	[PMID: 31560541]
A549	IC₅₀	0.14 μM Compound: AZD9291	Antiproliferative activity against human A549 cells measured after 72 hrs by sulforhodamine B assay Antiproliferative activity against human A549 cells measured after 72 hrs by sulforhodamine B assay	[PMID: 31889606]
A549	IC₅₀	0.31 μM Compound: 2	Cytotoxicity against human A549 cells assessed as cell growth inhibition after 4 days by CCK-8 assay Cytotoxicity against human A549 cells assessed as cell growth inhibition after 4 days by CCK-8 assay	[PMID: 30108918]
A549	IC₅₀	0.335 μM Compound: Osimertinib	Antiproliferative activity against human A549 cells expressing wild type EGFR assessed as inhibition in cell viability after 72 hrs by CCK8 assay Antiproliferative activity against human A549 cells expressing wild type EGFR assessed as inhibition in cell viability after 72 hrs by CCK8 assay	[PMID: 34794818]
A549	IC₅₀	0.445 μM Compound: Osimertinib	Antiproliferative activity against human A549 cells expressing wild type EGFR incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human A549 cells expressing wild type EGFR incubated for 72 hrs by CCK-8 assay	[PMID: 35691176]
A549	IC₅₀	0.462 μM Compound: 3; AZD9291	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth after 72 hrs by MTT assay	[PMID: 31683104]
A549	IC₅₀	0.53 μM Compound: osimertinib	Cytotoxicity against human A549 cells harboring wild type EGFR assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human A549 cells harboring wild type EGFR assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 29853340]
A549	IC₅₀	0.53 μM Compound: AZD	Antiproliferative activity against human A549 cells harboring wild type EGFR after 72 hrs by MTT assay Antiproliferative activity against human A549 cells harboring wild type EGFR after 72 hrs by MTT assay	[PMID: 29466773]
A549	IC₅₀	0.615 μM Compound: 6; AZD9291	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 30530173]
A549	IC₅₀	0.67 μM Compound: AZD9291	Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 32679450]
A549	IC₅₀	0.672 μM Compound: AZD9291	Cytotoxicity against human A549 cells assessed as reduction in cell viability measured by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell viability measured by MTT assay	[PMID: 34534838]
A549	IC₅₀	0.72 μM Compound: 4	Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay	[PMID: 31787359]
A549	IC₅₀	0.784 μM Compound: AZD9291	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 35447433]
A549	IC₅₀	0.87 μM Compound: AZD9291	Cytotoxicity against human A549 cells expressing wild-type EGFR/K-ras mutant after 72 hrs by MTT assay Cytotoxicity against human A549 cells expressing wild-type EGFR/K-ras mutant after 72 hrs by MTT assay	[PMID: 29486953]
A549	IC₅₀	0.9 μM Compound: Osimertinib	Antiproliferative activity against human A549 cells harboring EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells harboring EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31951960]
A549	IC₅₀	1.557 nM Compound: Osimertinib	Antiproliferative activity against human A549 cells expressing wild type EGFR assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay Antiproliferative activity against human A549 cells expressing wild type EGFR assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay	[PMID: 37087886]
A549	EC₅₀	1.83 μM Compound: Osimertinib	Antiproliferative activity against human A549 cells harboring KRAS-G12S mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay Antiproliferative activity against human A549 cells harboring KRAS-G12S mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay	[PMID: 28853575]
A549	IC₅₀	1.87 μM Compound: 3	Antiproliferative activity against human A549 cells assessed as cell viability after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 35696862]
A549	IC₅₀	1.97 μM Compound: Osimertinib	Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay	[PMID: 32961382]
A549	IC₅₀	150 nM Compound: 9; AZD9291	Inhibition of EGF-stimulated wild type EGFR autophosphorylation expressed in human A549 cells by sandwich ELISA Inhibition of EGF-stimulated wild type EGFR autophosphorylation expressed in human A549 cells by sandwich ELISA	[PMID: 26756222]
A549	IC₅₀	3.242 μM Compound: 6; AZD-9291	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 30471829]
A549	GI₅₀	3.5 μM Compound: 5; AZD9291	Inhibition of wild-type EGFR in human A549 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay Inhibition of wild-type EGFR in human A549 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay	[PMID: 28282122]
A549	IC₅₀	486 nM Compound: AZD9291	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 29576272]
A549	IC₅₀	5 μM Compound: Osimertinib	Antiproliferative activity against wild type human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against wild type human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31446247]
ASPC1	IC₅₀	3.985 μM Compound: 6; AZD-9291	Antiproliferative activity against human Aspc-1 cells after 72 hrs by MTT assay Antiproliferative activity against human Aspc-1 cells after 72 hrs by MTT assay	[PMID: 30471829]
BaF3	IC₅₀	> 1 μM Compound: 65, AZD9291	Antiproliferative activity against mouse BA/F3 cells expressing TEL-JAK3 after 72 hrs by cell titer glo assay Antiproliferative activity against mouse BA/F3 cells expressing TEL-JAK3 after 72 hrs by cell titer glo assay	[PMID: 26258521]
BaF3	IC₅₀	> 3000 nM Compound: 4	Cytotoxicity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay Cytotoxicity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay	[PMID: 34464874]
BaF3	EC₅₀	> 5000 nM Compound: Osimertinib	Antiproliferative activity against mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay Antiproliferative activity against mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 28528303]
BaF3	IC₅₀	0.033 μM Compound: Osimertinib	Antiproliferative activity against mouse BaF3 cells harboring EGFR del19/T790M double mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring EGFR del19/T790M double mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 36064123]
BaF3	GI₅₀	0.347 μM Compound: Osimertinib	Antiproliferative activity against mouse Ba/F3 cells harbouring Her2-A775_G776insYVMA mutant measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against mouse Ba/F3 cells harbouring Her2-A775_G776insYVMA mutant measured after 72 hrs by CellTiter-Glo assay	[PMID: 35486541]
BaF3	EC₅₀	0.545 μM Compound: Osimertinib	Antiproliferative activity against mouse Ba/F3 cells harbouring Her2-A775_G776insYVMA mutant measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against mouse Ba/F3 cells harbouring Her2-A775_G776insYVMA mutant measured after 72 hrs by CellTiter-Glo assay	[PMID: 35486541]
BaF3	IC₅₀	0.859 μM Compound: Osimertinib	Antiproliferative activity against mouse BaF3 cells harboring EGFR del19/T790M/C797S triple mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring EGFR del19/T790M/C797S triple mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 36064123]
BaF3	IC₅₀	1 nM Compound: Osimertinib	Inhibition of EGFR del19 mutant in mouse BAF3 cells incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay Inhibition of EGFR del19 mutant in mouse BAF3 cells incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay	[PMID: 31689114]
BaF3	GI₅₀	1.2 μM Compound: 5; AZD9291	Growth inhibition of mouse BAF3 cells after 72 hrs by CellTiter-Glo assay Growth inhibition of mouse BAF3 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28282122]
BaF3	IC₅₀	10.1 nM Compound: Osimertinib	Antiproliferative activity against mouse BaF3 cells expressing L858R/T790M assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing L858R/T790M assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
BaF3	IC₅₀	110 nM Compound: AZD9291	Antiproliferative activity against mouse BaF3 cells expressing wild type EGFR incubated for 72 hrs in absence of cetuximab by Cell Titer-Glo assay Antiproliferative activity against mouse BaF3 cells expressing wild type EGFR incubated for 72 hrs in absence of cetuximab by Cell Titer-Glo assay	[PMID: 34668706]
BaF3	IC₅₀	1100 nM Compound: Osimertinib	Cytotoxicity against mouse BAF3 cells incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay Cytotoxicity against mouse BAF3 cells incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay	[PMID: 31689114]
BaF3	IC₅₀	1200 nM Compound: AZD9291	Antiproliferative activity against mouse BaF3 cells expressing EGFR Ex19del/T790M/C797S mutant incubated for 72 hrs in absence of cetuximab by Cell Titer-Glo assay Antiproliferative activity against mouse BaF3 cells expressing EGFR Ex19del/T790M/C797S mutant incubated for 72 hrs in absence of cetuximab by Cell Titer-Glo assay	[PMID: 34668706]
BaF3	IC₅₀	1320.5 nM Compound: Osimertinib	Antiproliferative activity against mouse BaF3 cells expressing De119/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing De119/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
BaF3	EC₅₀	14 nM Compound: AZD9291	Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R/T790M mutant after 72 hrs by resazurin dye-based fluorescence assay Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R/T790M mutant after 72 hrs by resazurin dye-based fluorescence assay	[PMID: 36518696]
BaF3	IC₅₀	1409.5 nM Compound: Osimertinib	Antiproliferative activity against mouse BaF3 cells expressing L858R/T790M/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing L858R/T790M/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
BaF3	IC₅₀	1475 nM Compound: Osimertinib	Antiproliferative activity against mouse BaF3 cells expressing L858R/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing L858R/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
BaF3	IC₅₀	1503.9 nM Compound: Osimertinib	Antiproliferative activity against mouse BaF3 cells expressing De119/T790M/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing De119/T790M/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
BaF3	IC₅₀	154.1 nM Compound: Osimertinib	Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion GV mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion GV mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
BaF3	IC₅₀	16 nM Compound: AZD9291	Antiproliferative activity against mouse BaF3 cells expressing wild type EGFR incubated for 72 hrs in presence of 1 ug/ml cetuximab by Cell Titer-Glo assay Antiproliferative activity against mouse BaF3 cells expressing wild type EGFR incubated for 72 hrs in presence of 1 ug/ml cetuximab by Cell Titer-Glo assay	[PMID: 34668706]
BaF3	EC₅₀	16 nM Compound: Osimertinib	Inhibition of EGFR T790M exon19 deletion double mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay Inhibition of EGFR T790M exon19 deletion double mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 28528303]
BaF3	EC₅₀	1748 nM Compound: Osimertinib	Inhibition of EML4/ALK (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay Inhibition of EML4/ALK (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 28528303]
BaF3	EC₅₀	18 nM Compound: Osimertinib	Inhibition of EGFR exon19 deletion mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay Inhibition of EGFR exon19 deletion mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 28528303]
BaF3	IC₅₀	2 nM Compound: AZD9291	Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M mutant incubated for 72 hrs in presence of 1 ug/ml cetuximab by Cell Titer-Glo assay Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M mutant incubated for 72 hrs in presence of 1 ug/ml cetuximab by Cell Titer-Glo assay	[PMID: 34668706]
BaF3	IC₅₀	2.5 nM Compound: Osimertinib	Antiproliferative activity against mouse BaF3 cells expressing L858R assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing L858R assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
BaF3	IC₅₀	2.885 μM Compound: AZD9291; 5	Antiproliferative activity against mouse BaF3 cells expressing EGFR 19Del/T790M/C797S triple mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing EGFR 19Del/T790M/C797S triple mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay	[PMID: 35178175]
BaF3	IC₅₀	2.893 μM Compound: AZD9291; 5	Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay	[PMID: 35178175]
BaF3	EC₅₀	20 nM Compound: Osimertinib	Inhibition of EGFR T790M/L858R double mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay Inhibition of EGFR T790M/L858R double mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 28528303]
BaF3	IC₅₀	21.5 nM Compound: AZD9291	Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M mutant incubated for 72 hrs by Cell Titer-Glo luminescent assay Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M mutant incubated for 72 hrs by Cell Titer-Glo luminescent assay	[PMID: 33459024]
BaF3	EC₅₀	2956 nM Compound: 1	Cytotoxicity against mouse BaF3 cells expressing EGFR L858R/C797S mutant assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay Cytotoxicity against mouse BaF3 cells expressing EGFR L858R/C797S mutant assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay	[PMID: 37197473]
BaF3	IC₅₀	3 nM Compound: AZD9291	Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R mutant incubated for 72 hrs in presence of 1 ug/ml cetuximab by Cell Titer-Glo assay Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R mutant incubated for 72 hrs in presence of 1 ug/ml cetuximab by Cell Titer-Glo assay	[PMID: 34668706]
BaF3	EC₅₀	3.2 nM Compound: AZD9291	Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R mutant after 72 hrs by resazurin dye-based fluorescence assay Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R mutant after 72 hrs by resazurin dye-based fluorescence assay	[PMID: 36518696]
BaF3	IC₅₀	3.3 nM Compound: AZD9291	Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R mutant incubated for 72 hrs in absence of cetuximab by Cell Titer-Glo assay Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R mutant incubated for 72 hrs in absence of cetuximab by Cell Titer-Glo assay	[PMID: 34668706]
BaF3	IC₅₀	3.52 μM Compound: 5	Cytotoxicity against mouse IL-3 dependent BaF3 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Cytotoxicity against mouse IL-3 dependent BaF3 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 35446588]
BaF3	IC₅₀	3.93 μM Compound: 4; AZD9291	Antiproliferative activity against mouse BAF3 cells transfected with EGFR L858R/T790M/C797S mutant (unknown origin) incubated for 72 hrs by resazurin dye based assay Antiproliferative activity against mouse BAF3 cells transfected with EGFR L858R/T790M/C797S mutant (unknown origin) incubated for 72 hrs by resazurin dye based assay	[PMID: 31223440]
BaF3	IC₅₀	300.1 nM Compound: Osimertinib	Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion SVD mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion SVD mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
BaF3	IC₅₀	3100 nM Compound: Osimertinib	Inhibition of phosphorylated EGFR del19/T790M/C797S triple mutant (unknown origin) expressed in mouse BaF3 cells incubated for 4 hrs by Alphascreen assay Inhibition of phosphorylated EGFR del19/T790M/C797S triple mutant (unknown origin) expressed in mouse BaF3 cells incubated for 4 hrs by Alphascreen assay	[PMID: 31689114]
BaF3	EC₅₀	34 nM Compound: AZD9291	Antiproliferative activity against mouse BAF3 cells harboring HER2 wild type after 72 hrs by resazurin dye-based fluorescence assay Antiproliferative activity against mouse BAF3 cells harboring HER2 wild type after 72 hrs by resazurin dye-based fluorescence assay	[PMID: 36518696]
BaF3	IC₅₀	4 nM Compound: AZD9291	Antiproliferative activity against mouse BaF3 cells harboring EGFR del19/T790M mutant incubated for 72 hrs by Cell Titer-Glo luminescent assay Antiproliferative activity against mouse BaF3 cells harboring EGFR del19/T790M mutant incubated for 72 hrs by Cell Titer-Glo luminescent assay	[PMID: 33459024]
BaF3	IC₅₀	4.27 μM Compound: 5	Antiproliferative activity against mouse BaF3 cells stably expressing EGFR L858R/T790M/C797S mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells stably expressing EGFR L858R/T790M/C797S mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 35446588]
BaF3	IC₅₀	4.3 nM Compound: Osimertinib	Antiproliferative activity against mouse BaF3 cells expressing Del19 assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing Del19 assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
BaF3	IC₅₀	4.427 μM Compound: AZD9291; 5	Antiproliferative activity against mouse BaF3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay	[PMID: 35178175]
BaF3	IC₅₀	4.5 nM Compound: Osimertinib	Antiproliferative activity against mouse BaF3 cells expressing De119/T790M assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing De119/T790M assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
BaF3	IC₅₀	4.61 μM Compound: AZD9291	Antiproliferative activity against mouse BAF3 cells harboring EGFR 19D/T790M/C797S mutant after 72 hrs by resazurin dye based assay Antiproliferative activity against mouse BAF3 cells harboring EGFR 19D/T790M/C797S mutant after 72 hrs by resazurin dye based assay	[PMID: 30429956]
BaF3	IC₅₀	5.11 μM Compound: 4; AZD9291	Cytotoxicity against mouse BAF3 cells incubated for 72 hrs by resazurin dye based assay Cytotoxicity against mouse BAF3 cells incubated for 72 hrs by resazurin dye based assay	[PMID: 31223440]
BaF3	IC₅₀	5.15 μM Compound: AZD9291	Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R/T790M/C797S mutant after 72 hrs by resazurin dye based assay Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R/T790M/C797S mutant after 72 hrs by resazurin dye based assay	[PMID: 30429956]
BaF3	IC₅₀	5.47 μM Compound: 6, AZD9291	Antiproliferative activity against mouse BAF3 cells harboring EGFR 19D/T790M/C797S mutant assessed as reduction in cell viability by CCK8 assay Antiproliferative activity against mouse BAF3 cells harboring EGFR 19D/T790M/C797S mutant assessed as reduction in cell viability by CCK8 assay	[PMID: 32631532]
BaF3	IC₅₀	53.1 nM Compound: Osimertinib	Antiproliferative activity against mouse BaF3 cells expressing EGFR WT assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing EGFR WT assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
BaF3	EC₅₀	6 nM Compound: 1	Cytotoxicity against mouse BaF3 cells expressing EGFR L858R mutant assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay Cytotoxicity against mouse BaF3 cells expressing EGFR L858R mutant assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay	[PMID: 37197473]
BaF3	EC₅₀	6 nM Compound: Osimertinib	Inhibition of EGFR L858R mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay Inhibition of EGFR L858R mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 28528303]
BaF3	IC₅₀	6.071 nM Compound: 5	Antiproliferative activity against mouse BaF3 cells harboring EGFR 19 del/T790M/C797S mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay Antiproliferative activity against mouse BaF3 cells harboring EGFR 19 del/T790M/C797S mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay	[PMID: 35446588]
BaF3	IC₅₀	60.6 nM Compound: Osimertinib	Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion NPG mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion NPG mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
BaF3	EC₅₀	66 nM Compound: Osimertinib	Inhibition of wild type EGFR (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay Inhibition of wild type EGFR (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay	[PMID: 28528303]
BaF3	IC₅₀	780 nM Compound: Osimertinib	Inhibition of EGFR del19/T790M/C797S triple mutant in mouse BAF3 cells assessed as reduction in cell proliferation incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay Inhibition of EGFR del19/T790M/C797S triple mutant in mouse BAF3 cells assessed as reduction in cell proliferation incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay	[PMID: 31689114]
BaF3	IC₅₀	8 nM Compound: AZD9291	Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M mutant incubated for 72 hrs in absence of cetuximab by Cell Titer-Glo assay Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M mutant incubated for 72 hrs in absence of cetuximab by Cell Titer-Glo assay	[PMID: 34668706]
BaF3	IC₅₀	800 nM Compound: AZD9291	Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M/C797S mutant incubated for 72 hrs in presence of 1 ug/ml cetuximab by Cell Titer-Glo assay Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M/C797S mutant incubated for 72 hrs in presence of 1 ug/ml cetuximab by Cell Titer-Glo assay	[PMID: 34668706]
BaF3	IC₅₀	81 nM Compound: Osimertinib	Inhibition of wild type EGFR in mouse BAF3 cells assessed as reduction in cell proliferation incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay Inhibition of wild type EGFR in mouse BAF3 cells assessed as reduction in cell proliferation incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay	[PMID: 31689114]
BEAS-2B	IC₅₀	14.9 μM Compound: 1; AZD9291	Antiproliferative activity against human BEAS2B cells after 72 hrs by MTS assay Antiproliferative activity against human BEAS2B cells after 72 hrs by MTS assay	[PMID: 28716641]
BJ	IC₅₀	> 10 μM Compound: AZD9291	Cytotoxicity against human BJ cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human BJ cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31581004]
Calu-3	IC₅₀	0.75 μM Compound: Osimertinib	Antiproliferative activity against human Calu3 cells harboring WT EGFR after 72 hrs by MTS assay Antiproliferative activity against human Calu3 cells harboring WT EGFR after 72 hrs by MTS assay	[PMID: 30442506]
Calu-3	GI₅₀	264 nM Compound: 8	Cytotoxicity against human Calu3 cells assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay Cytotoxicity against human Calu3 cells assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay	[PMID: 25271963]
Calu-6	IC₅₀	5.86 μM Compound: Osimertinib	Antiproliferative activity against human Calu6 cells harboring WT EGFR after 72 hrs by MTS assay Antiproliferative activity against human Calu6 cells harboring WT EGFR after 72 hrs by MTS assay	[PMID: 30442506]
CHO	GI₅₀	4.2 μM Compound: 5; AZD9291	Growth inhibition of CHO cells after 72 hrs by CellTiter-Glo assay Growth inhibition of CHO cells after 72 hrs by CellTiter-Glo assay	[PMID: 28282122]
CL97	IC₅₀	0.1 μM Compound: Osimertinib	Antiproliferative activity against human CL97 cells harbouring EGFR G719A/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human CL97 cells harbouring EGFR G719A/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31446247]
EA.hy 926	IC₅₀	1.161 μM Compound: Osimertinib	Cytotoxicity against human EA.hy 926 cells assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay Cytotoxicity against human EA.hy 926 cells assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay	[PMID: 37087886]
HaCaT	IC₅₀	73.7 nM Compound: 5; AZD9291	Inhibition of wild type EGFR phosphorylation in human HaCaT cells incubated for 3 hrs by ELISA method Inhibition of wild type EGFR phosphorylation in human HaCaT cells incubated for 3 hrs by ELISA method	[PMID: 27433829]
HCC827	EC₅₀	< 0.014 μM Compound: Osimertinib	Antiproliferative activity against human HCC827 cells harboring EGFR-delE746_A750 mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay Antiproliferative activity against human HCC827 cells harboring EGFR-delE746_A750 mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay	[PMID: 28853575]
HCC827	IC₅₀	0.00173 μM Compound: Osimertinib	Antiproliferative activity against human HCC827 cells expressing EGFR del119 mutant assessed as inhibition in cell viability after 72 hrs by CCK8 assay Antiproliferative activity against human HCC827 cells expressing EGFR del119 mutant assessed as inhibition in cell viability after 72 hrs by CCK8 assay	[PMID: 34794818]
HCC827	IC₅₀	0.00248 μM Compound: Osimertinib	Antiproliferative activity against human NCI-HCC827 cells expressing EGFR del19 incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human NCI-HCC827 cells expressing EGFR del19 incubated for 72 hrs by CCK-8 assay	[PMID: 35691176]
HCC827	IC₅₀	0.003 μM Compound: 4	Antiproliferative activity against human HCC827 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells incubated for 72 hrs by MTT assay	[PMID: 31787359]
HCC827	IC₅₀	0.011 μM Compound: Osimertinib	Antiproliferative activity against human HCC827 cells harboring EGFR mutant after 72 hrs by MTS assay Antiproliferative activity against human HCC827 cells harboring EGFR mutant after 72 hrs by MTS assay	[PMID: 30442506]
HCC827	IC₅₀	0.027 μM Compound: osimertinib	Antiproliferative activity against human HCC827 cells harboring EGFR E746 to A750 deletion mutant after 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells harboring EGFR E746 to A750 deletion mutant after 72 hrs by MTT assay	[PMID: 29853340]
HCC827	IC₅₀	0.027 μM Compound: AZD	Antiproliferative activity against human HCC827 cells harboring EGFR E746-A750 deletion mutant after 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells harboring EGFR E746-A750 deletion mutant after 72 hrs by MTT assay	[PMID: 29466773]
HCC827	IC₅₀	0.036 μM Compound: Osimertinib	Antiproliferative activity against human HCC827 cells harboring EGFRDel19 mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells harboring EGFRDel19 mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31951960]
HCC827	IC₅₀	0.2 μM Compound: AZD9291	Antiproliferative activity against human HCC827 cells measured after 72 hrs by sulforhodamine B assay Antiproliferative activity against human HCC827 cells measured after 72 hrs by sulforhodamine B assay	[PMID: 31889606]
HCC827	IC₅₀	0.97 nM Compound: AZD9291	Antiproliferative activity against human HCC827 cells expressing EGFR del19 mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells expressing EGFR del19 mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 32883633]
HCC827	IC₅₀	1 nM Compound: Osimertinib	Antiproliferative activity against human HCC827 cells expressing EGFR deletion19 mutant assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells expressing EGFR deletion19 mutant assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 35254067]
HCC827	IC₅₀	25.4 nM Compound: AZD9291	Antiproliferative activity against human HCC827 cells after 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells after 72 hrs by MTT assay	[PMID: 29576272]
HEK293	IC₅₀	0.57 μM Compound: AZD9291	Inhibition of human ERG expressed in HEK293 cells by lonWorks Quattro analysis Inhibition of human ERG expressed in HEK293 cells by lonWorks Quattro analysis	[PMID: 28426996]
HEK293-A	IC₅₀	2.418 μM Compound: AZD9291	Cytotoxicity against human HEK293A cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human HEK293A cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31581004]
HeLa	IC₅₀	0.975 μM Compound: 3; AZD9291	Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth after 72 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth after 72 hrs by MTT assay	[PMID: 31683104]
HeLa	IC₅₀	1.83 μM Compound: AZD9291	Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 32679450]
HepG2	IC₅₀	1.605 μM Compound: 6; AZD9291	Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay	[PMID: 30530173]
HK-2	IC₅₀	2.399 μM Compound: Osimertinib	Cytotoxicity against human HK-2 cells assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay Cytotoxicity against human HK-2 cells assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay	[PMID: 37087886]
HK-2	IC₅₀	2.719 μM Compound: AZD9291	Cytotoxicity against HK-2 cells assessed as reduction in cell viability by MTT assay Cytotoxicity against HK-2 cells assessed as reduction in cell viability by MTT assay	[PMID: 33429247]
HK-2	IC₅₀	3.565 μM Compound: AZD9291	Cytotoxicity against human HK2 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human HK2 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31581004]
HT-29	IC₅₀	0.65 μM Compound: AZD9291	Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 29486953]
HUVEC	IC₅₀	7.278 μM Compound: AZD9291	Cytotoxicity against HUVEC assessed as reduction in cell viability measured after 72 hrs by Celltiter-Glo luminescent cell viability assay Cytotoxicity against HUVEC assessed as reduction in cell viability measured after 72 hrs by Celltiter-Glo luminescent cell viability assay	[PMID: 32619886]
KG-1	IC₅₀	0.53 μM Compound: Osimertinib	Antiproliferative activity against human KG-1 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human KG-1 cells incubated for 72 hrs by MTT assay	[PMID: 32961382]
L02	IC₅₀	> 40 μM Compound: Osimertinib	Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 33640672]
L02	IC₅₀	> 50 μM Compound: AZD9291	Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 32679450]
L02	IC₅₀	0.3 μM Compound: AZD9291	Cytotoxicity against human HL7702 cells measured after 72 hrs by sulforhodamine B assay Cytotoxicity against human HL7702 cells measured after 72 hrs by sulforhodamine B assay	[PMID: 31889606]
L02	IC₅₀	1.602 μM Compound: AZD9291	Cytotoxicity against human LO2 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human LO2 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31581004]
L02	IC₅₀	1.975 μM Compound: AZD9291	Cytotoxicity against human L02 cells assessed as reduction in cell viability by MTT assay Cytotoxicity against human L02 cells assessed as reduction in cell viability by MTT assay	[PMID: 33429247]
LoVo	IC₅₀	480 nM Compound: AZD9291	Inhibition of wild type EGFR phosphorylation in human LoVo cells preincubated for 2 hrs followed by EGF stimulation measured after 30 mins by ELISA Inhibition of wild type EGFR phosphorylation in human LoVo cells preincubated for 2 hrs followed by EGF stimulation measured after 30 mins by ELISA	[PMID: 26968253]
LoVo	IC₅₀	480 μM Compound: 8	Inhibition of wild type EGFR phosphorylation in human LoVo cells after 2 hrs by fluorescence assay Inhibition of wild type EGFR phosphorylation in human LoVo cells after 2 hrs by fluorescence assay	[PMID: 25271963]
MCF7	IC₅₀	3.67 μM Compound: AZD9291	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 32679450]
MDA-MB-468	IC₅₀	1.3 μM Compound: Osimertinib	Antiproliferative activity against human MDA-MB-468 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-468 cells incubated for 72 hrs by MTT assay	[PMID: 32961382]
NCI-H1299	IC₅₀	> 10 μM Compound: AZD9291; 5	Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell proliferation measured after 72 hrs by SRB assay Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell proliferation measured after 72 hrs by SRB assay	[PMID: 35178175]
NCI-H1299	IC₅₀	2.84 μM Compound: Osimertinib	Antiproliferative activity against human NCI-H1299 cells expressing wild type EGFR assessed as inhibition in cell viability after 72 hrs by CCK8 assay Antiproliferative activity against human NCI-H1299 cells expressing wild type EGFR assessed as inhibition in cell viability after 72 hrs by CCK8 assay	[PMID: 34794818]
NCI-H1299	IC₅₀	3.24 μM Compound: Osimertinib	Antiproliferative activity against human NCI-H1299 cells expressing wild type EGFR incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human NCI-H1299 cells expressing wild type EGFR incubated for 72 hrs by CCK-8 assay	[PMID: 35691176]
NCI-H1975	EC₅₀	< 0.014 μM Compound: Osimertinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR-L858R/T790M double mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR-L858R/T790M double mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay	[PMID: 28853575]
NCI-H1975	IC₅₀	< 1 μM Compound: 4	Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell growth by MTT assay Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell growth by MTT assay	[PMID: 31869655]
NCI-H1975	IC₅₀	0.011 nM Compound: AZD9291	Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R mutant by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R mutant by MTT assay	[PMID: 33429247]
NCI-H1975	IC₅₀	0.012 μM Compound: 4	Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay	[PMID: 31787359]
NCI-H1975	IC₅₀	0.013 μM Compound: 2	Cytotoxicity against human NCI-H1975 cells assessed as cell growth inhibition after 4 days by CCK-8 assay Cytotoxicity against human NCI-H1975 cells assessed as cell growth inhibition after 4 days by CCK-8 assay	[PMID: 30108918]
NCI-H1975	IC₅₀	0.014 μM Compound: AZD9291	Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31581004]
NCI-H1975	IC₅₀	0.0148 μM Compound: Osimertinib	Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant assessed as inhibition in cell viability after 72 hrs by CCK-8 assay Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant assessed as inhibition in cell viability after 72 hrs by CCK-8 assay	[PMID: 34794818]
NCI-H1975	IC₅₀	0.016 μM Compound: 1	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability measured after 72 hrs by WST assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability measured after 72 hrs by WST assay	[PMID: 32550993]
NCI-H1975	IC₅₀	0.019 nM Compound: Osimertinib	Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/ L858R double mutant assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/ L858R double mutant assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay	[PMID: 37087886]
NCI-H1975	EC₅₀	0.019 μM Compound: Osimertinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as growth inhibition after 96 hrs by CellTiter-Glo assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as growth inhibition after 96 hrs by CellTiter-Glo assay	[PMID: 28603991]
NCI-H1975	IC₅₀	0.019 μM Compound: osimertinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay	[PMID: 29853340]
NCI-H1975	IC₅₀	0.019 μM Compound: AZD	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay	[PMID: 29466773]
NCI-H1975	IC₅₀	0.023 μM Compound: AZD-9291	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by MTT assay	[PMID: 29534926]
NCI-H1975	IC₅₀	0.03 μM Compound: 4; AZD9291	Antiproliferative activity human NCI-H1975 cells incubated for 72 hrs by SRB assay Antiproliferative activity human NCI-H1975 cells incubated for 72 hrs by SRB assay	[PMID: 31223440]
NCI-H1975	IC₅₀	0.03 μM Compound: 3	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by SRB assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by SRB assay	[PMID: 28033579]
NCI-H1975	IC₅₀	0.0305 μM Compound: Osimertinib	Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M incubated for 72 hrs by CCK-8 assay	[PMID: 35691176]
NCI-H1975	IC₅₀	0.041 μM Compound: 5; AZD9291	Antiproliferative activity against EGFR T790M/L858R double mutant expressing human NCI-H1975 cells after 72 hrs by SRB assay Antiproliferative activity against EGFR T790M/L858R double mutant expressing human NCI-H1975 cells after 72 hrs by SRB assay	[PMID: 29730192]
NCI-H1975	IC₅₀	0.044 μM Compound: Osimertinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31951960]
NCI-H1975	IC₅₀	0.05 μM Compound: Osimertinib	Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M double mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M double mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31446247]
NCI-H1975	IC₅₀	0.052 μM Compound: AZD9291	Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant after 72 hrs by SRB assay Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant after 72 hrs by SRB assay	[PMID: 27131639]
NCI-H1975	IC₅₀	0.06 μM Compound: Osimertinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTS assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTS assay	[PMID: 30442506]
NCI-H1975	IC₅₀	0.06 μM Compound: AZD9291	Cytotoxicity against human NCI-H1975 cells expressing EGFR L858R/T790M double mutant after 72 hrs by MTT assay Cytotoxicity against human NCI-H1975 cells expressing EGFR L858R/T790M double mutant after 72 hrs by MTT assay	[PMID: 29486953]
NCI-H1975	IC₅₀	0.064 μM Compound: 3; AZD9291	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell proliferation incubated for 72 hrs by sulforhodamine B colorimetric assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell proliferation incubated for 72 hrs by sulforhodamine B colorimetric assay	[PMID: 28987609]
NCI-H1975	IC₅₀	0.07 μM Compound: Osimertinib	Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTS assay Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTS assay	[PMID: 31718182]
NCI-H1975	IC₅₀	0.072 μM Compound: 3	Antiproliferative activity against human H1975 cells assessed as cell viability after 72 hrs by MTT assay Antiproliferative activity against human H1975 cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 35696862]
NCI-H1975	IC₅₀	0.073 μM Compound: 3; AZD9291	Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as inhibition of cell growth after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as inhibition of cell growth after 72 hrs by MTT assay	[PMID: 31683104]
NCI-H1975	IC₅₀	0.073 μM Compound: 6; AZD9291	Antiproliferative activity against human NCI-H1975 cells after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells after 72 hrs by MTT assay	[PMID: 30530173]
NCI-H1975	IC₅₀	0.076 μM Compound: AZD9291	Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell viability measured by MTT assay Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell viability measured by MTT assay	[PMID: 34534838]
NCI-H1975	IC₅₀	0.091 μM Compound: AZD9291	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay	[PMID: 34218082]
NCI-H1975	IC₅₀	0.095 μM Compound: 4	Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R mutant assessed as reduction in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R mutant assessed as reduction in cell growth incubated for 72 hrs by MTT assay	[PMID: 36288657]
NCI-H1975	IC₅₀	0.096 μM Compound: 6; AZD-9291	Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTT assay	[PMID: 30471829]
NCI-H1975	IC₅₀	0.1 μM Compound: AZD9291	Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M mutant assessed as reduction in cell viability measured after 72 hrs by CCK8 assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M mutant assessed as reduction in cell viability measured after 72 hrs by CCK8 assay	[PMID: 35178185]
NCI-H1975	IC₅₀	0.1 μM Compound: 4	Growth inhibition of human NCI-H1975 cells after 72 hrs by MTT assay Growth inhibition of human NCI-H1975 cells after 72 hrs by MTT assay	[PMID: 30472599]
NCI-H1975	IC₅₀	0.125 μM Compound: 1	Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36173763]
NCI-H1975	IC₅₀	0.13 μM Compound: AZD9291	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by resazurin dye based assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by resazurin dye based assay	[PMID: 30429956]
NCI-H1975	IC₅₀	0.74 μM Compound: 6, AZD9291	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability by CCK8 assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability by CCK8 assay	[PMID: 32631532]
NCI-H1975	IC₅₀	0.98 μM Compound: Osimertinib	Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 33640672]
NCI-H1975	IC₅₀	10.5 nM Compound: 1; AZD9291	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTS assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTS assay	[PMID: 28716641]
NCI-H1975	IC₅₀	15 nM Compound: 9; AZD9291	Inhibition of EGFR L858R/T790M double mutant autophosphorylation in human NCI-H1975 cells after 2 hrs by sandwich ELISA Inhibition of EGFR L858R/T790M double mutant autophosphorylation in human NCI-H1975 cells after 2 hrs by sandwich ELISA	[PMID: 26756222]
NCI-H1975	IC₅₀	15 μM Compound: 8	Inhibition of EGFR L858R/T970M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay Inhibition of EGFR L858R/T970M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay	[PMID: 25271963]
NCI-H1975	IC₅₀	17 nM Compound: Osimertinib	Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 35254067]
NCI-H1975	IC₅₀	18.21 nM Compound: AZD9291	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant measured after 72 hrs by celltiter-glo assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant measured after 72 hrs by celltiter-glo assay	[PMID: 33667898]
NCI-H1975	IC₅₀	2.08 μM Compound: Osimertinib	Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs under hypoxic condition by MTT assay Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs under hypoxic condition by MTT assay	[PMID: 33640672]
NCI-H1975	GI₅₀	2.8 nM Compound: Osimertinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTS assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTS assay	[PMID: 30442506]
NCI-H1975	GI₅₀	24 nM Compound: 8	Cytotoxicity against human NCI-H1975 cells harboring EGFR L858R/T970M double mutant assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay Cytotoxicity against human NCI-H1975 cells harboring EGFR L858R/T970M double mutant assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay	[PMID: 25271963]
NCI-H1975	IC₅₀	3.1 μM Compound: Osimertinib	Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M/C797S mutant incubated for 72 hrs by MTS assay Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M/C797S mutant incubated for 72 hrs by MTS assay	[PMID: 31718182]
NCI-H1975	IC₅₀	3.85 μM Compound: 1	Antiproliferative activity against human NCI-H1975 cells harbouring wild type Akt3 assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human NCI-H1975 cells harbouring wild type Akt3 assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36173763]
NCI-H1975	IC₅₀	4.32 μM Compound: 1	Antiproliferative activity against human NCI-H1975 cells harbouring Akt3 T305A/S472A mutant assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human NCI-H1975 cells harbouring Akt3 T305A/S472A mutant assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 36173763]
NCI-H1975	IC₅₀	42 nM Compound: AZD9291	Antiproliferative activity against human H1975 cells expressing EGFR L858R/T790M mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against human H1975 cells expressing EGFR L858R/T790M mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 32883633]
NCI-H1975	IC₅₀	47.2 nM Compound: AZD9291	Antiproliferative activity against human NCI-H1975 cells after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells after 72 hrs by MTT assay	[PMID: 29576272]
NCI-H1975	IC₅₀	47.3 nM Compound: AZD9291	Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay	[PMID: 33459024]
NCI-H1975	IC₅₀	73.4 nM Compound: AZD9291	Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as inhibition of cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as inhibition of cell viability measured after 72 hrs by MTT assay	[PMID: 32679450]
NCI-H292	IC₅₀	0.22 μM Compound: 1	Antiproliferative activity against human NCI-H292 cells expressing wild type EGFR assessed as reduction in cell viability measured after 72 hrs by WST assay Antiproliferative activity against human NCI-H292 cells expressing wild type EGFR assessed as reduction in cell viability measured after 72 hrs by WST assay	[PMID: 32550993]
NCI-H292	IC₅₀	0.924 nM Compound: AZD9291	Antiproliferative activity against human NCI-H292 cells harboring wild-type EGFR by MTT assay Antiproliferative activity against human NCI-H292 cells harboring wild-type EGFR by MTT assay	[PMID: 33429247]
NCI-H292	IC₅₀	1.084 μM Compound: AZD9291	Antiproliferative activity against human NCI-H292 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H292 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31581004]
NCI-H460	IC₅₀	415.9 nM Compound: 1; AZD9291	Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTS assay Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTS assay	[PMID: 28716641]
PC-9	IC₅₀	< 0.01 μM Compound: Osimertinib	Antiproliferative activity against human PC9 cells harbouring EGFR delE746-A750 mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human PC9 cells harbouring EGFR delE746-A750 mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31446247]
PC-9	IC₅₀	> 1000 nM Compound: Osimertinib	Antiproliferative activity against human PC9 cells harboring EGFR del19/T790M/C797S triple mutant incubated for 96 hrs by Celltiter-Glo luminescent cell viability assay Antiproliferative activity against human PC9 cells harboring EGFR del19/T790M/C797S triple mutant incubated for 96 hrs by Celltiter-Glo luminescent cell viability assay	[PMID: 31689114]
PC-9	IC₅₀	0.011 nM Compound: AZD9291	Antiproliferative activity against human PC-9 cells harboring EGFR L858R mutant by MTT assay Antiproliferative activity against human PC-9 cells harboring EGFR L858R mutant by MTT assay	[PMID: 33429247]
PC-9	IC₅₀	0.011 μM Compound: AZD9291; 5	Antiproliferative activity against human PC-9 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay Antiproliferative activity against human PC-9 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay	[PMID: 35178175]
PC-9	IC₅₀	0.016 μM Compound: AZD9291	Antiproliferative activity against human PC9 cells expressing EGFR L858R mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human PC9 cells expressing EGFR L858R mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31581004]
PC-9	IC₅₀	0.023 nM Compound: Osimertinib	Antiproliferative activity against human PC-9 cells expressing EGFR Del19 mutant assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay Antiproliferative activity against human PC-9 cells expressing EGFR Del19 mutant assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay	[PMID: 37087886]
PC-9	IC₅₀	0.16 μM Compound: Osimertinib	Antiproliferative activity against human PC9 cells harboring EGFR mutant after 72 hrs by MTS assay Antiproliferative activity against human PC9 cells harboring EGFR mutant after 72 hrs by MTS assay	[PMID: 30442506]
PC-9	IC₅₀	17 nM Compound: AZD9291	Inhibition of EGFR Del ex19 mutant phosphorylation in human PC9 cells preincubated for 2 hrs by ELISA Inhibition of EGFR Del ex19 mutant phosphorylation in human PC9 cells preincubated for 2 hrs by ELISA	[PMID: 26968253]
PC-9	IC₅₀	17 μM Compound: 8	Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assay Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assay	[PMID: 25271963]
PC-9	GI₅₀	23 nM Compound: 8	Cytotoxicity against human PC9 cells harboring EGFR exon 19 deletion activating mutant assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay Cytotoxicity against human PC9 cells harboring EGFR exon 19 deletion activating mutant assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay	[PMID: 25271963]
PC-9	IC₅₀	3.21 μM Compound: AZD9291; 5	Antiproliferative activity against human PC-9 cells expressing EGFR 19Del/T790M/C797S triple mutation assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay Antiproliferative activity against human PC-9 cells expressing EGFR 19Del/T790M/C797S triple mutation assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay	[PMID: 35178175]
PC-9	IC₅₀	3.248 μM Compound: AZD9291	Antiproliferative activity against human PC-9 cells expressing EGFR L858R/T790M/C797S mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human PC-9 cells expressing EGFR L858R/T790M/C797S mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 35447433]
PC-9	IC₅₀	5.431 nM Compound: 5	Antiproliferative activity against human osimertinib-resistant PC-9 cells harboring EGFR 19 del/T790M/C797S mutant assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human osimertinib-resistant PC-9 cells harboring EGFR 19 del/T790M/C797S mutant assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 35446588]
PC-9	IC₅₀	56 nM Compound: 9; AZD9291	Inhibition of EGFR deletion mutant autophosphorylation in human PC9 cells after 2 hrs by sandwich ELISA Inhibition of EGFR deletion mutant autophosphorylation in human PC9 cells after 2 hrs by sandwich ELISA	[PMID: 26756222]
PC-9	IC₅₀	6.5 nM Compound: 1; AZD9291	Antiproliferative activity against human PC9 cells harboring EGFR exon 19 deletion mutant after 72 hrs by MTS assay Antiproliferative activity against human PC9 cells harboring EGFR exon 19 deletion mutant after 72 hrs by MTS assay	[PMID: 28716641]
Sf9	IC₅₀	0.002 μM Compound: Osimertinib	Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR L858R/T790M double mutant (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo k Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR L858R/T790M double mutant (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo k	[PMID: 31718182]
Sf9	IC₅₀	0.09 μM Compound: Osimertinib	Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR L858R/T790M/C797S mutant (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo ki Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR L858R/T790M/C797S mutant (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo ki	[PMID: 31718182]
Sf9	IC₅₀	1.23 μM Compound: Osimertinib	Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo kinase assay Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo kinase assay	[PMID: 31718182]
Sf9	IC₅₀	20.8 nM Compound: 6; AZD-9291	Inhibition of human N-terminal GST-tagged EGFR T790M/L858R double mutant (695 to end residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate after 60 mins in presence of ATP by ADP-Glo assay Inhibition of human N-terminal GST-tagged EGFR T790M/L858R double mutant (695 to end residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate after 60 mins in presence of ATP by ADP-Glo assay	[PMID: 30471829]
Sf9	IC₅₀	567.5 nM Compound: 6; AZD-9291	Inhibition of wild-type human N-terminal GST-tagged EGFR (695 to end residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate after 60 mins in presence of ATP by ADP-Glo assay Inhibition of wild-type human N-terminal GST-tagged EGFR (695 to end residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate after 60 mins in presence of ATP by ADP-Glo assay	[PMID: 30471829]
U-87MG ATCC	IC₅₀	4.5 μM Compound: 4	Antiproliferative activity against human U-87MG cells harboring wild type EGFR assessed as inhibition of cell growth by MTT assay Antiproliferative activity against human U-87MG cells harboring wild type EGFR assessed as inhibition of cell growth by MTT assay	[PMID: 31869655]
Vero	CC₅₀	13.23 μM Compound: Osimertinib	Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr	10.1101/2020.03.20.999730
Vero	IC₅₀	3.26 μM Compound: Osimertinib	Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr	10.1101/2020.03.20.999730

In Vitro

Osimertinib (AZD9291) (0-10 μM; 72 hours) dramatically inhibits cell proliferation with IC₅₀s of 41, 26, 41, and 31 nM, respectively^[2].
? Osimertinib (0-10 μM; 72 hours) inhibits cell proliferation (Ba/F3 cells harboring a T790M mutation, exon 19del+T790M, or L858R+T790M) with IC₅₀s of 6, 7, and 74 nM, respectively^[2].
? Osimertinib (0-10 μM; 72 hours) inhibits Ba/F3 cells harboring EGFR exon 20 insertion mutations (IC₅₀ ranging from 16 to 701 nM for A763_Y764insFQEA (FQEA), Y764_V765insHH (HH), A767_V769dupASV (ASV), and D770_N771insNPG (NPG) cells)^[2].
? Osimertinib shows high levels of phenotype potency in both sensitizing-mutant (mean IC₅₀ of 8 nM in PC-9) and T790M (mean IC₅₀s of 11 and 40 nM in H1975 and PC-9VanR respectively) EGFR cell lines. Osimertinib has much less activity towards wild-type EGFR (mean IC₅₀s of 650 and 461 nM in Calu3 and H2073 respectively)^[1].
? Osimertinib (0.1 μM; 48 hours) induces apoptosis in Ba/F3 cells (apoptosis rates of 40.9% and 90% in EGFR exon 19del+T790M, EGFR L858R+T790M respectively) ^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[2]

Cell Line:	Ba/F3 cells (harboring a T790M mutation, exon 19del+T790M, or L858R+T790M)
Concentration:	0.0001, 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time:	72 hours
Result:	Inhibited cell proliferation (IC₅₀s=6, 7, 74 nM, respectively)

Cell Proliferation Assay^[2]

Cell Line:	PC-9, H3255, PC-9ER, and H1975 cells
Concentration:	0.0001, 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time:	72 hours
Result:	Dramatically inhibited cell proliferation (IC₅₀s=41, 26, 41, 31 nM, respectively)

Cell Proliferation Assay^[2]

Cell Line:	Ba/F3 cells (harboring EGFR exon 20 insertion mutations: FQEA, HH, ASV, NPG )
Concentration:	0.0001, 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time:	72 hours
Result:	Inhibited cell proliferation (IC₅₀s=16, 701, 230, 38 nM, respectively)

Apoptosis Analysis^[2]

Cell Line:	Ba/F3 cells (harboring EGFR exon 19del+T790M or EGFR L858R+T790M)
Concentration:	0.1 μM
Incubation Time:	48 hours
Result:	Induced apoptosis with the rates of 40.9% and 90% in EGFR T790M positive mutations cells, respectively.

In Vivo

Osimertinib (0.1-25 mg/kg; p.o.; daily for 14 days) induces significant dose-dependent regression in both PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models^[1]
Dosage:	0.1-10 mg/kg (PC-9 xenograft models); 0.5- 25 mg/kg (H1975 xenograft models)
Administration:	p.o.; daily for 14 days
Result:	Induced significant dose-dependent regression in both PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models.

Clinical Trial

Molecular Weight

499.61

Formula

C₂₈H₃₃N₇O₂

CAS No.

1421373-65-0

Appearance

Solid

Color

Light yellow to brown

SMILES

C=CC(NC1=CC(NC2=NC=CC(C3=CN(C)C4=C3C=CC=C4)=N2)=C(OC)C=C1N(CCN(C)C)C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (200.16 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.0016 mL	10.0078 mL	20.0156 mL
5 mM	0.4003 mL	2.0016 mL	4.0031 mL
10 mM	0.2002 mL	1.0008 mL	2.0016 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.00 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 2

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.5 mg/mL (5.00 mM); Clear solution
Protocol 3

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.16 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 0.5% HPMC/1% Tween-80 in Saline water
Solubility: 5 mg/mL (10.01 mM); Suspened solution; Need ultrasonic and warming and heat to 60°C

Purity & Documentation

Purity: 99.96%

Data Sheet (284 KB) SDS (393 KB)

COA (0 KB) LCMS (0 KB) Elemental Analysis Report (113 KB)

Handling Instructions (2659 KB)

References

[1]. Cross DA, et al. AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer. Cancer Discov. 2014 Sep;4(9):1046-61. [Content Brief]

[2]. Hirano T, et al. Pharmacological and Structural Characterizations of Naquotinib, a Novel Third-Generation EGFR Tyrosine Kinase Inhibitor, in EGFR-Mutated Non-Small Cell Lung Cancer. Mol Cancer Ther. 2018 Apr;17(4):740-750. [Content Brief]

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