Vemurafenib [918504-65-1]

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Vémurafénib (PLX4032) est un inhibiteurde la B-RAF kinase qui est puissant, sélectif et de première classe, avec la IC50s de 31 et 48 nM pour RAFV600E et c-RAF-1, respectivement. Vémurafénib induit une autophagie cellulaire.

Vemurafenib (PLX4032; RG7204; RO5185426) ist ein erstklassiger, selektiver, potenter Inhibitor der B-RAF-Kinase mit IC50s-Werten von 31 bzw. 48 nM für RAFV600E und c-RAF-1. Vemurafenib induziert die autophagy.

Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAFV600E and c-RAF-1, respectively. Vemurafenib induces cell autophagy.

For research use only. We do not sell to patients.

Vemurafenib Chemical Structure

Vemurafenib Chemical Structure

CAS No. : 918504-65-1

This product is a controlled substance and not for sale in your territory.

Based on 84 publication(s) in Google Scholar

Other Forms of Vemurafenib:

  • Vemurafenib-d5 Get quote
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  • Vemurafenib (Standard) Get quote

    Vemurafenib purchased from MedChemExpress. Usage Cited in: EBioMedicine. 2019 Jan;39:194-206.  [Abstract]

    Western analysis of related proteins expression with or without the treatment of vemurafenib and other treatments. Left: M6 are transfected with PLAUR siRNA and negative control siRNA and incubated for 48 h in presence of 1 μM vemurafenib. Right: A375 are transfected either with Mock or uPAR overexpressing plasmid pQ2-uPAR. After 24 h are seeded at the same density (800 cells/ml) and cultured in the presence of vemurafenib at indicated concentrations for 10 days.

    Vemurafenib purchased from MedChemExpress. Usage Cited in: Int J Cancer. 2019 Mar 15;144(6):1379-1390.  [Abstract]

    Western blot confirmed increased MAPK pathway activity in NEC-DUE2 cells when compared to NECDUE1. Treatment with Vemurafenib (1 μM), GSK2118436A (100 nM), or GSK1120212 (100 nM) for 4 hours leads to decreased MAPK signaling in NEC-DUE2 cells. Lysates are immunoblotted for the proteins indicated.

    Vemurafenib purchased from MedChemExpress. Usage Cited in: Oncogene. 2018 Oct;37(43):5719-5734.  [Abstract]

    BRAF mutants with in-frame β3-αC loop deletions exhibit a robust but differential inhibitor resistance. Stable fibroblast cells that express individual BRAF mutants with in-frame β3-αC loop deletions are treated with Vemurafenib for 4 h, and p-ERK1/2 is probed by immunoblot and quantified.

    Vemurafenib purchased from MedChemExpress. Usage Cited in: Nutrients. 2018 Dec 8;10(12). pii: E1950.  [Abstract]

    Western analysis of protein expression in cells treatmented with or without PLX4032 or RAD001.

    Vemurafenib purchased from MedChemExpress. Usage Cited in: Mol Syst Biol. 2017 Jan; 13(1): 905.  [Abstract]

    Western blotting for NGFR-inducible COLO858 cells, NGFRHigh A375 and WM115 cells, and NGFRLow MACSF and MZ7MEL cells, treated for 48 h with 0.2 or 1 μM Vmurafenib or DMSO.

    Vemurafenib purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2017 Nov 1;408:43-54.  [Abstract]

    Western blot analysis of p-ERK, ERK, p-AKT and ERK after 24 h of treatment with Vemurafenib. Levels of p-ERK and p-AKT are quantified by densitometric analysis and a corresponding histogram is constructed as relative to ERK or AKT and α-tubulin. Representative Western blot panels on the left.

    Vemurafenib purchased from MedChemExpress. Usage Cited in: J Mol Med (Berl). 2017 Jan;95(1):97-108.  [Abstract]

    Immunoblotting of phosphorylated and total EGFR,AKT, and ERK1/2 in A375-M6 clones treated or not with 0.5 μMvemurafenib for 24 h. 50 μL/ well loaded. Tubulin detected as loading control. Quantification (right) of phosphorylated protein on total protein, normalized on housekeeper (Tubulin).

    Vemurafenib purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2013 Feb 1;19(3):598-609.  [Abstract]

    MEKi decreases PD-L1 expression in BRAFi-resistant cells. A, immunoblot analyses of the activities of ERK1/2 and c-Jun in the K028, M34, and K029 parental lines treated with U0126 (U; 20 μM), PLX4032 (PLX; 10 μM), or the combination of U0126 (20 μM) and PLX4032 (10 μM) for 30 minutes. Cells are treated with DMSO (D) as controls. B, immunoblot example showing decrease in PD-L1 expression in parental M34 cells treated with U0126, PLX4032, or the combination.

    View All Raf Isoform Specific Products:

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    BRaf c-Raf Raf
    Description

    Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAFV600E and c-RAF-1, respectively[1][4]. Vemurafenib induces cell autophagy[5].

    IC50 & Target[1]

    B-RafV600E

    31 nM (IC50)

    c-Raf-1

    48 nM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    A-375 IC50
    > 10000 nM
    Compound: 1
    Competitive binding affinity to CRAF in human A375 cells after 15 mins in presence of ATP analogue
    Competitive binding affinity to CRAF in human A375 cells after 15 mins in presence of ATP analogue
    [PMID: 25965804]
    A-375 IC50
    0.079 μM
    Compound: 1
    Antiproliferative activity against human A375 cells expressing B-Raf V600E mutant incubated for 68 hrs by MTT assay
    Antiproliferative activity against human A375 cells expressing B-Raf V600E mutant incubated for 68 hrs by MTT assay
    [PMID: 26005530]
    A-375 IC50
    0.15 μM
    Compound: 1
    Inhibition of BRAF V600E mutant in human A375 cells assessed as inhibition of ERK phosphorylation measured after 72 hrs by ELISA assay
    Inhibition of BRAF V600E mutant in human A375 cells assessed as inhibition of ERK phosphorylation measured after 72 hrs by ELISA assay
    [PMID: 25965804]
    A-375 IC50
    0.17 μM
    Compound: 1
    Antiproliferative activity against human A375 cells after 72 hrs by resazurin assay
    Antiproliferative activity against human A375 cells after 72 hrs by resazurin assay
    [PMID: 25965804]
    A-375 IC50
    0.18 μM
    Compound: Vemurafenib
    Cytotoxicity against human A375 cells after 72 hrs by MTT assay
    Cytotoxicity against human A375 cells after 72 hrs by MTT assay
    [PMID: 24215818]
    A-375 IC50
    0.19 μM
    Compound: PLX4032
    Antiproliferative activity against human A375 cells after 48 hrs by MTT assay
    Antiproliferative activity against human A375 cells after 48 hrs by MTT assay
    [PMID: 25267006]
    A-375 IC50
    0.21 μM
    Compound: PLX4032
    Antiproliferative activity against human A375 cells assessed as cell growth inhibition after 24 hrs by MTT assay
    Antiproliferative activity against human A375 cells assessed as cell growth inhibition after 24 hrs by MTT assay
    [PMID: 27634195]
    A-375 IC50
    0.7 μM
    Compound: Vemurafenib
    Antiproliferative activity human A375 cells after 72 hrs by cell titer-glo luminescence assay
    Antiproliferative activity human A375 cells after 72 hrs by cell titer-glo luminescence assay
    [PMID: 28242553]
    A-375 IC50
    0.7 μM
    Compound: Vemurafenib
    Antiproliferative activity against human A375 cells after 72 hrs by Cell-Titer Glo assay
    Antiproliferative activity against human A375 cells after 72 hrs by Cell-Titer Glo assay
    [PMID: 30529543]
    A-375 GI50
    0.95 μM
    Compound: Vemurafenib
    Antiproliferative activity against human A375 cells after 48 hrs by MTT assay
    Antiproliferative activity against human A375 cells after 48 hrs by MTT assay
    [PMID: 29940463]
    A-375 IC50
    116 nM
    Compound: 1
    Cytotoxicity in human A375 cells assessed as reduction in cell viability by Cell-titer-Lumi assay
    Cytotoxicity in human A375 cells assessed as reduction in cell viability by Cell-titer-Lumi assay
    [PMID: 32223235]
    A-375 IC50
    127 nM
    Compound: Vem
    Antiproliferative activity at human A375 cells expressing BRAF V600E mutant assessed as reduction in cell viability incubated for 96 hrs by MTT assay
    Antiproliferative activity at human A375 cells expressing BRAF V600E mutant assessed as reduction in cell viability incubated for 96 hrs by MTT assay
    [PMID: 31312411]
    A-375 IC50
    17 nM
    Compound: 2
    Inhibition of B-Raf V600E mutant in human A375 cells assessed as ERK phosphorylation preincubated for 1 hr by Western blot method
    Inhibition of B-Raf V600E mutant in human A375 cells assessed as ERK phosphorylation preincubated for 1 hr by Western blot method
    [PMID: 27085672]
    A-375 IC50
    190 nM
    Compound: 1, PLX4032
    Inhibition of B-Raf V600E mutant-mediated Erk phosphorylation in human A375 cells after 1 hr by fluorescence analysis
    Inhibition of B-Raf V600E mutant-mediated Erk phosphorylation in human A375 cells after 1 hr by fluorescence analysis
    [PMID: 24900315]
    A-375 IC50
    260 nM
    Compound: 1
    Competitive binding affinity to BRAF in human A375 cells after 15 mins in presence of ATP analogue
    Competitive binding affinity to BRAF in human A375 cells after 15 mins in presence of ATP analogue
    [PMID: 25965804]
    A-375 IC50
    3.315 μM
    Compound: 1, PLX4032
    Antiproliferative activity against human A375 cells after 72 hrs by CCK8 assay
    Antiproliferative activity against human A375 cells after 72 hrs by CCK8 assay
    [PMID: 25462267]
    A-375 IC50
    33.1 nM
    Compound: 1, PLX4032
    Inhibition of B-raf V600E mutant in human A375 cells assessed as reduction in ERK1/2 phosphorylation incubated for 90 mins by Western blotting method
    Inhibition of B-raf V600E mutant in human A375 cells assessed as reduction in ERK1/2 phosphorylation incubated for 90 mins by Western blotting method
    [PMID: 25462267]
    A-375 IC50
    5.9 μM
    Compound: Vemurafenib
    Cytotoxicity against human A-375 cells by MTT assay
    Cytotoxicity against human A-375 cells by MTT assay
    [PMID: 33316752]
    A-375 IC50
    81 nM
    Compound: Vemurafenib
    Cytotoxicity against human A375 cells assessed as decrease in cell viability after 72 hrs by CellTiter-Glo luminescence assay
    Cytotoxicity against human A375 cells assessed as decrease in cell viability after 72 hrs by CellTiter-Glo luminescence assay
    [PMID: 26844689]
    A-375 IC50
    950 nM
    Compound: 1
    Competitive binding affinity to ARAF in human A375 cells after 15 mins in presence of ATP analogue
    Competitive binding affinity to ARAF in human A375 cells after 15 mins in presence of ATP analogue
    [PMID: 25965804]
    CHL-1 IC50
    > 50 μM
    Compound: PLX-4032
    Antiproliferative activity against human CHL-1 cells harboring wild type BRAF after 24 hrs by MTT assay
    Antiproliferative activity against human CHL-1 cells harboring wild type BRAF after 24 hrs by MTT assay
    [PMID: 28458134]
    CHL-1 IC50
    12.7 μM
    Compound: PLX-4032
    Antiproliferative activity against human CHL-1 cells harboring wild type BRAF after 72 hrs by MTT assay
    Antiproliferative activity against human CHL-1 cells harboring wild type BRAF after 72 hrs by MTT assay
    [PMID: 28458134]
    CHL-1 IC50
    13.7 μM
    Compound: PLX-4032
    Antiproliferative activity against human CHL-1 cells harboring wild type BRAF after 72 hrs by MTT assay
    Antiproliferative activity against human CHL-1 cells harboring wild type BRAF after 72 hrs by MTT assay
    [PMID: 29133035]
    CHL-1 IC50
    20 μM
    Compound: PLX-4032
    Antiproliferative activity against human CHL-1 cells harboring wild type BRAF after 48 hrs by MTT assay
    Antiproliferative activity against human CHL-1 cells harboring wild type BRAF after 48 hrs by MTT assay
    [PMID: 28458134]
    COLO 205 IC50
    0.044 μM
    Compound: 1
    Cytotoxicity against human COLO205 cells harboring B-Raf V600E mutant assessed as growth inhibition after 72 hrs by MTT assay
    Cytotoxicity against human COLO205 cells harboring B-Raf V600E mutant assessed as growth inhibition after 72 hrs by MTT assay
    [PMID: 27155899]
    COLO 205 IC50
    0.309 μM
    Compound: 1
    Antiproliferative activity against human COLO205 cells expressing B-Raf V600E mutant incubated for 68 hrs by MTT assay
    Antiproliferative activity against human COLO205 cells expressing B-Raf V600E mutant incubated for 68 hrs by MTT assay
    [PMID: 26005530]
    COLO 205 EC50
    240 nM
    Compound: 1, PLX4032
    Cytotoxicity against human COLO205 cells after 4 days by CellTiter-Glo assay
    Cytotoxicity against human COLO205 cells after 4 days by CellTiter-Glo assay
    [PMID: 24900315]
    COLO 205 IC50
    5.16 μM
    Compound: Vemurafenib
    Antiproliferative activity human COLO205 cells after 72 hrs by cell titer-glo luminescence assay
    Antiproliferative activity human COLO205 cells after 72 hrs by cell titer-glo luminescence assay
    [PMID: 28242553]
    HCT-116 IC50
    > 10 μM
    Compound: 1
    Antiproliferative activity against human HCT116 cells expressing wild type B-Raf incubated for 68 hrs by MTT assay
    Antiproliferative activity against human HCT116 cells expressing wild type B-Raf incubated for 68 hrs by MTT assay
    [PMID: 26005530]
    HCT-116 IC50
    > 10 μM
    Compound: 1
    Antiproliferative activity against human HCT116 cells after 67 hrs by resazurin assay
    Antiproliferative activity against human HCT116 cells after 67 hrs by resazurin assay
    [PMID: 25965804]
    HCT-116 IC50
    > 30 μM
    Compound: Vemurafenib
    Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay
    Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay
    [PMID: 24215818]
    HCT-116 IC50
    14.58 μM
    Compound: 1
    Cytotoxicity against human HCT116 cells harboring wild type B-Raf assessed as growth inhibition after 72 hrs by MTT assay
    Cytotoxicity against human HCT116 cells harboring wild type B-Raf assessed as growth inhibition after 72 hrs by MTT assay
    [PMID: 27155899]
    HCT-116 IC50
    16.6 μM
    Compound: 1
    Inhibition of KRAS G13D mutant in human HCT116 cells assessed as inhibition of ERK phosphorylation by ELISA
    Inhibition of KRAS G13D mutant in human HCT116 cells assessed as inhibition of ERK phosphorylation by ELISA
    [PMID: 25965804]
    HCT-116 GI50
    25.2 μM
    Compound: Vemurafenib
    Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay
    Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay
    [PMID: 29940463]
    HEK-293T CC50
    > 50 μM
    Compound: PLX4032
    Cytotoxicity against human 293T cells assessed as cell growth inhibition after 24 hrs by MTT assay
    Cytotoxicity against human 293T cells assessed as cell growth inhibition after 24 hrs by MTT assay
    [PMID: 27634195]
    HepG2 IC50
    5.48 μM
    Compound: Vemurafenib
    Antiproliferative activity human HepG2 cells after 72 hrs by cell titer-glo luminescence assay
    Antiproliferative activity human HepG2 cells after 72 hrs by cell titer-glo luminescence assay
    [PMID: 28242553]
    HepG2 IC50
    5.5 μM
    Compound: Vemurafenib
    Antiproliferative activity against human HepG2 cells after 72 hrs by Cell-Titer Glo assay
    Antiproliferative activity against human HepG2 cells after 72 hrs by Cell-Titer Glo assay
    [PMID: 30529543]
    HT-29 IC50
    0.156 μM
    Compound: 1
    Cytotoxicity against human HT-29 cells harboring B-Raf V600E mutant assessed as growth inhibition after 72 hrs by MTT assay
    Cytotoxicity against human HT-29 cells harboring B-Raf V600E mutant assessed as growth inhibition after 72 hrs by MTT assay
    [PMID: 27155899]
    HT-29 IC50
    0.601 μM
    Compound: 1
    Antiproliferative activity against human HT-29 cells expressing B-Raf V600E mutant incubated for 68 hrs by MTT assay
    Antiproliferative activity against human HT-29 cells expressing B-Raf V600E mutant incubated for 68 hrs by MTT assay
    [PMID: 26005530]
    HT-29 GI50
    1.88 μM
    Compound: Vemurafenib
    Antiproliferative activity against human HT-29 cells after 48 hrs by MTT assay
    Antiproliferative activity against human HT-29 cells after 48 hrs by MTT assay
    [PMID: 29940463]
    HT-29 GI50
    100 nM
    Compound: PLX4032
    Antiproliferative activity against human HT-29 cells incubated for 3 days by WST8 assay
    Antiproliferative activity against human HT-29 cells incubated for 3 days by WST8 assay
    [PMID: 33284613]
    HT-29 IC50
    164 nM
    Compound: 1
    Cytotoxicity in human HT-29 cells assessed as reduction in cell viability by Cell-titer-Lumi assay
    Cytotoxicity in human HT-29 cells assessed as reduction in cell viability by Cell-titer-Lumi assay
    [PMID: 32223235]
    HT-29 IC50
    4.9 μM
    Compound: Vemurafenib
    Antiproliferative activity against human HT-29 cells after 72 hrs by Cell-Titer Glo assay
    Antiproliferative activity against human HT-29 cells after 72 hrs by Cell-Titer Glo assay
    [PMID: 30529543]
    LoVo IC50
    > 10 μM
    Compound: 1
    Antiproliferative activity against human LoVo cells expressing wild type B-Raf incubated for 68 hrs by MTT assay
    Antiproliferative activity against human LoVo cells expressing wild type B-Raf incubated for 68 hrs by MTT assay
    [PMID: 26005530]
    Malme-3M IC50
    61 nM
    Compound: 1, PLX4032
    Inhibition of B-Raf V600E mutant-mediated Erk phosphorylation in human MALME-3M cells after 1 hr by fluorescence analysis
    Inhibition of B-Raf V600E mutant-mediated Erk phosphorylation in human MALME-3M cells after 1 hr by fluorescence analysis
    [PMID: 24900315]
    MIA PaCa-2 EC50
    2290 nM
    Compound: 2
    Inhibition of wild type B-Raf in human MIAPaCa2 cells assessed as reduction in ERK phosphorylation preincubated for 1 hr by Western blot method
    Inhibition of wild type B-Raf in human MIAPaCa2 cells assessed as reduction in ERK phosphorylation preincubated for 1 hr by Western blot method
    [PMID: 27085672]
    SK-MEL-1 IC50
    1.499 μM
    Compound: 1
    Antiproliferative activity against human SK-MEL-1 cells expressing B-Raf V600E mutant incubated for 68 hrs by MTT assay
    Antiproliferative activity against human SK-MEL-1 cells expressing B-Raf V600E mutant incubated for 68 hrs by MTT assay
    [PMID: 26005530]
    SK-MEL-2 IC50
    > 10 μM
    Compound: 1
    Antiproliferative activity against human SK-MEL-2 cells expressing wild type B-Raf incubated for 68 hrs by MTT assay
    Antiproliferative activity against human SK-MEL-2 cells expressing wild type B-Raf incubated for 68 hrs by MTT assay
    [PMID: 26005530]
    SK-MEL-2 IC50
    5.6 μM
    Compound: Vemurafenib
    Antiproliferative activity against human SK-MEL-2 cells after 72 hrs by Cell-Titer Glo assay
    Antiproliferative activity against human SK-MEL-2 cells after 72 hrs by Cell-Titer Glo assay
    [PMID: 30529543]
    SK-MEL-2 IC50
    5.64 μM
    Compound: Vemurafenib
    Antiproliferative activity human SK-MEL-2 cells after 72 hrs by cell titer-glo luminescence assay
    Antiproliferative activity human SK-MEL-2 cells after 72 hrs by cell titer-glo luminescence assay
    [PMID: 28242553]
    SK-MEL-28 IC50
    0.381 μM
    Compound: 1
    Antiproliferative activity against human SK-MEL-28 cells expressing B-Raf V600E mutant incubated for 68 hrs by MTT assay
    Antiproliferative activity against human SK-MEL-28 cells expressing B-Raf V600E mutant incubated for 68 hrs by MTT assay
    [PMID: 26005530]
    SK-MEL-28 IC50
    0.48 μM
    Compound: 1, PLX4032
    Antiproliferative activity against human SK-MEL-28 cells harboring BRAF V600E mutant after 68 hrs by MTS assay
    Antiproliferative activity against human SK-MEL-28 cells harboring BRAF V600E mutant after 68 hrs by MTS assay
    [PMID: 24588073]
    UACC-903 IC50
    > 50 μM
    Compound: PLX-4032
    Antiproliferative activity against human UACC-903 cells harboring BRAF V600E mutant after 24 hrs by MTT assay
    Antiproliferative activity against human UACC-903 cells harboring BRAF V600E mutant after 24 hrs by MTT assay
    [PMID: 28458134]
    UACC-903 IC50
    12.3 μM
    Compound: PLX-4032
    Antiproliferative activity against human UACC-903 cells harboring BRAF V600E mutant after 48 hrs by MTT assay
    Antiproliferative activity against human UACC-903 cells harboring BRAF V600E mutant after 48 hrs by MTT assay
    [PMID: 28458134]
    UACC-903 IC50
    2.7 μM
    Compound: PLX-4032
    Antiproliferative activity against human UACC-903 cells harboring BRAF V600E mutant after 72 hrs by MTT assay
    Antiproliferative activity against human UACC-903 cells harboring BRAF V600E mutant after 72 hrs by MTT assay
    [PMID: 28458134]
    UACC-903 IC50
    3.6 μM
    Compound: PLX-4032
    Cytotoxicity against human UACC-903 cells assessed as cell viability at 25 uM after 48 hrs by MTT assay relative to control
    Cytotoxicity against human UACC-903 cells assessed as cell viability at 25 uM after 48 hrs by MTT assay relative to control
    [PMID: 29133035]
    WM 266-4 IC50
    0.06 μM
    Compound: PLX4032
    Antiproliferative activity against human WM266.4 cells after 48 hrs by MTT assay
    Antiproliferative activity against human WM266.4 cells after 48 hrs by MTT assay
    [PMID: 25267006]
    WM 266-4 IC50
    0.07 μM
    Compound: PLX4032
    Antiproliferative activity against human WM266.4 cells harboring BRAF V600E mutant assessed as cell growth inhibition after 24 hrs by MTT assay
    Antiproliferative activity against human WM266.4 cells harboring BRAF V600E mutant assessed as cell growth inhibition after 24 hrs by MTT assay
    [PMID: 27634195]
    WM 266-4 GI50
    0.21 μM
    Compound: Vemurafenib
    Antiproliferative activity against human WM266.4 cells assessed as cell viability after 24 hrs by MTT assay
    Antiproliferative activity against human WM266.4 cells assessed as cell viability after 24 hrs by MTT assay
    [PMID: 27238841]
    WM 266-4 GI50
    0.21 μM
    Compound: Vemurafenib
    Antiproliferative activity against human WM266.4 cells after 48 hrs by MTT assay
    Antiproliferative activity against human WM266.4 cells after 48 hrs by MTT assay
    [PMID: 29940463]
    In Vitro

    Vemurafenib (PLX4032) selectively blocks the RAF/MEK/ERK pathway in BRAF mutant cells[1]. RG7204 is a potent inhibitor of proliferation in those expressing RAFV600E but not BRAFWT in 17 melanoma cell lines. Vemurafenib (RG7204) induces MEK and ERK phosphorylation at high concentrations in CHL-1 cells[2]. Ectopic expression of EGFR in melanoma cells is sufficient to cause resistance to PLX4032[3].

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

    In Vivo

    Vemurafenib (PLX4032, 20, 25, 75 mg/kg, p.o.) causes dose-dependent inhibition of tumor growth, with higher exposures resulting in tumor regression of BRAF mutant xenografts[1]. RG7204 (12.5, 25, and 75 mg/kg, p.o.) significantly inhibits tumor growth and induced tumor regression in mice bearing LOX tumor xenografts[2].

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

    Clinical Trial
    Molecular Weight

    489.92

    Formula

    C23H18ClF2N3O3S

    CAS No.

    918504-65-1

    Appearance

    Solid

    Color

    White to gray

    SMILES

    FC1=CC=C(C(F)=C1C(C2=CNC3=NC=C(C=C32)C4=CC=C(C=C4)Cl)=O)NS(CCC)(=O)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (102.06 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 2.0411 mL 10.2057 mL 20.4115 mL
    5 mM 0.4082 mL 2.0411 mL 4.0823 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    ×
    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

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    In Vivo:

    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    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (4.25 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.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.08 mg/mL (4.25 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

    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:  1.5% CMC-Na/saline water

      Solubility: 3.33 mg/mL (6.80 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.85%

    References
    • [1]. Bollag G, et al. Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma. Nature, 2010, 467(7315), 596-599.  [Content Brief]

      [2]. Yang H, et al. RG7204 (PLX4032), a selective BRAFV600E inhibitor, displays potent antitumor activity in preclinical melanoma models. Cancer Res, 2010, 70(13), 5518-5527.  [Content Brief]

      [3]. Prahallad A, et al. Unresponsiveness of colon cancer to BRAF(V600E) inhibition through feedback activation of EGFR. Nature, 2012, 483(7387), 100-103.  [Content Brief]

      [4]. Shelledy L, et al. Vemurafenib: First-in-Class BRAF-Mutated Inhibitor for the Treatment of Unresectable or MetastaticMelanoma. J Adv Pract Oncol. 2015 Jul-Aug;6(4):361-5.  [Content Brief]

      [5]. Wang W, et al. Targeting Autophagy Sensitizes BRAF-Mutant Thyroid Cancer to Vemurafenib.J Clin Endocrinol Metab. 2017 Feb 1;102(2):634-643.  [Content Brief]

    Cell Assay
    [2]

    Briefly, cells are plated in 96-well microtiter plates at a density of 1,000 to 5,000 cells per well in a volume of 180 μL. For the assay, Vemurafenib (RG7204) is prepared at 10 times the final assay concentration in media containing 1% DMSO. Twenty-four hours after cell plating, 20 μL of the appropriate dilution are added to plates in duplicate. The plates are assayed for proliferation 6 days after the cells are plated according to the procedure.

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

    Animal Administration
    [2]

    Athymic nude mice, are with ages 13 to 14 weeks, and weighing approximately 23 to 25 g. For the LOX xenografts, 2×106 cells in 0.2 mL of PBS are injected s.c. into the right lateral flank. Vemurafenib (RG7204), formulated as MBP, is suspended at the desired concentration as needed for each dose group in an aqueous vehicle containing 2% Klucel LF and adjusted to pH 4 with dilute HCl. NSC 362856 is of 250-mg capsules. Capsules are opened and combined into one bulk supply. To prepare the stock dosing material, NSC 362856 is first dissolved in 100% DMSO followed by dilution with saline to form a final milky white suspension in 10% DMSO/90% saline (pH 3.4).

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

    References
    • [1]. Bollag G, et al. Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma. Nature, 2010, 467(7315), 596-599.  [Content Brief]

      [2]. Yang H, et al. RG7204 (PLX4032), a selective BRAFV600E inhibitor, displays potent antitumor activity in preclinical melanoma models. Cancer Res, 2010, 70(13), 5518-5527.  [Content Brief]

      [3]. Prahallad A, et al. Unresponsiveness of colon cancer to BRAF(V600E) inhibition through feedback activation of EGFR. Nature, 2012, 483(7387), 100-103.  [Content Brief]

      [4]. Shelledy L, et al. Vemurafenib: First-in-Class BRAF-Mutated Inhibitor for the Treatment of Unresectable or MetastaticMelanoma. J Adv Pract Oncol. 2015 Jul-Aug;6(4):361-5.  [Content Brief]

      [5]. Wang W, et al. Targeting Autophagy Sensitizes BRAF-Mutant Thyroid Cancer to Vemurafenib.J Clin Endocrinol Metab. 2017 Feb 1;102(2):634-643.  [Content Brief]

    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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.0411 mL 10.2057 mL 20.4115 mL 51.0287 mL
    5 mM 0.4082 mL 2.0411 mL 4.0823 mL 10.2057 mL
    10 mM 0.2041 mL 1.0206 mL 2.0411 mL 5.1029 mL
    15 mM 0.1361 mL 0.6804 mL 1.3608 mL 3.4019 mL
    20 mM 0.1021 mL 0.5103 mL 1.0206 mL 2.5514 mL
    25 mM 0.0816 mL 0.4082 mL 0.8165 mL 2.0411 mL
    30 mM 0.0680 mL 0.3402 mL 0.6804 mL 1.7010 mL
    40 mM 0.0510 mL 0.2551 mL 0.5103 mL 1.2757 mL
    50 mM 0.0408 mL 0.2041 mL 0.4082 mL 1.0206 mL
    60 mM 0.0340 mL 0.1701 mL 0.3402 mL 0.8505 mL
    80 mM 0.0255 mL 0.1276 mL 0.2551 mL 0.6379 mL
    100 mM 0.0204 mL 0.1021 mL 0.2041 mL 0.5103 mL
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    Vemurafenib Related Classifications

    Help & FAQs

    Keywords:

    Vemurafenib918504-65-1PLX4032 RG7204 RO5185426PLX 4032PLX-4032RG7204RG 7204RG-7204RO5185426RO 5185426RO-5185426RafAutophagyRaf kinasesInhibitorinhibitorinhibit

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