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

Carfilzomib [868540-17-4]

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Cat# HY-10455-5mg

Size : 5mg

Brand : MedChemExpress

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Description

Carfilzomib (PR-171) is an irreversible proteasome inhibitor with an IC₅₀ of 5 nM in ANBL-6 and RPMI 8226 cells.

IC₅₀ & Target

IC50: 5 nM (Proteasome)

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	23.8 nM Compound: Carfilzomib	Antiproliferative activity against human A431 cells after 72 hrs by oxyluciferin luminescence assay Antiproliferative activity against human A431 cells after 72 hrs by oxyluciferin luminescence assay	[PMID: 26231162]
A549	IC₅₀	43.3 nM Compound: Carfilzomib	Antiproliferative activity against human A549 cells after 72 hrs by MTS assay Antiproliferative activity against human A549 cells after 72 hrs by MTS assay	[PMID: 30639896]
CCRF-CEM	IC₅₀	6.1 nM Compound: Carfilzomib	Antiproliferative activity against human CCRF-CEM cells after 72 hrs by oxyluciferin luminescence assay Antiproliferative activity against human CCRF-CEM cells after 72 hrs by oxyluciferin luminescence assay	[PMID: 26231162]
HCT-116	IC₅₀	19.3 nM Compound: Carfilzomib	Antiproliferative activity against human HCT116 cells after 72 hrs by oxyluciferin luminescence assay Antiproliferative activity against human HCT116 cells after 72 hrs by oxyluciferin luminescence assay	[PMID: 26231162]
HCT-116	IC₅₀	9.6 nM Compound: Carfilzomib	Antiproliferative activity against human HCT116 cells after 72 hrs by MTS assay Antiproliferative activity against human HCT116 cells after 72 hrs by MTS assay	[PMID: 30639896]
LP-1	IC₅₀	22.7 nM Compound: Carfilzomib	Antiproliferative activity against human LP-1 cells after 72 hrs by MTS assay Antiproliferative activity against human LP-1 cells after 72 hrs by MTS assay	[PMID: 30639896]
MCF7	IC₅₀	0.0041 μM Compound: Cfz	Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 30165344]
MDA-MB-231	IC₅₀	0.0044 μM Compound: Cfz	Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay	[PMID: 30165344]
MES-SA	IC₅₀	18 nM Compound: 2	Cytotoxicity against human MESSA cells assessed as cell viability after 72 hrs by CellTiter-Glo luminescent assay Cytotoxicity against human MESSA cells assessed as cell viability after 72 hrs by CellTiter-Glo luminescent assay	[PMID: 19348473]
MES-SA	IC₅₀	413 nM Compound: 2	Cytotoxicity against multidrug resistance transporter expressing doxorubicin resistant human MESSA cells assessed as cell viability after 72 hrs by CellTiter-Glo luminescent assay Cytotoxicity against multidrug resistance transporter expressing doxorubicin resistant human MESSA cells assessed as cell viability after 72 hrs by CellTiter-Glo luminescent assay	[PMID: 19348473]
MGC-803	IC₅₀	934 nM Compound: Carfilzomib	Antiproliferative activity against human MGC803 cells after 72 hrs by MTS assay Antiproliferative activity against human MGC803 cells after 72 hrs by MTS assay	[PMID: 30639896]
MM1.S	IC₅₀	< 1 nM Compound: 2	Antiproliferative activity against human MM1S cells after 72 hrs by MTS assay Antiproliferative activity against human MM1S cells after 72 hrs by MTS assay	[PMID: 30611983]
MM1.S	IC₅₀	1.5 nM Compound: Carfilzomib	Cytotoxicity against human MM1S cells measured after 72 hrs by MTS assay Cytotoxicity against human MM1S cells measured after 72 hrs by MTS assay	[PMID: 28027531]
MM1.S	IC₅₀	1.5 nM Compound: Carfilzomib	Antiproliferative activity against human MM1S cells measured after 72 hrs by MTS assay Antiproliferative activity against human MM1S cells measured after 72 hrs by MTS assay	[PMID: 27765408]
MM1.S	IC₅₀	14.35 nM Compound: Carfilzomib	Antiproliferative activity against human MM1.S cells assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against human MM1.S cells assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 33223460]
MM1.S	IC₅₀	2.3 nM Compound: Carfilzomib	Antiproliferative activity against human MM1S cells after 72 hrs by MTS assay Antiproliferative activity against human MM1S cells after 72 hrs by MTS assay	[PMID: 30639896]
MOLT-4	IC₅₀	5.1 nM Compound: 2	Inhibition of chymotrypsin-like activity of 20S proteasome in human MOLT4 cells after 1 hr by CellTiter-Glo luminescent assay Inhibition of chymotrypsin-like activity of 20S proteasome in human MOLT4 cells after 1 hr by CellTiter-Glo luminescent assay	[PMID: 19348473]
NCI-H23	IC₅₀	0.018 μM Compound: Cfz	Cytotoxicity against human NCI-H23 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay Cytotoxicity against human NCI-H23 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay	[PMID: 30964987]
NCI-H727	IC₅₀	0.6102 μM Compound: Cfz	Cytotoxicity against human NCI-H727 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay Cytotoxicity against human NCI-H727 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay	[PMID: 30964987]
NCI-H929	IC₅₀	116.1 nM Compound: Carfilzomib	Antiproliferative activity against human NCI-H929 cells after 72 hrs by MTS assay Antiproliferative activity against human NCI-H929 cells after 72 hrs by MTS assay	[PMID: 30639896]
NCI-H929	IC₅₀	13.9 nM Compound: Carfilzomib	Antiproliferative activity against human NCI-H929 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against human NCI-H929 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 33223460]
NCI-H929	IC₅₀	21.32 nM Compound: Carfilzomib	Cytotoxic activity against human NCI-H929 cells after 72 hrs by MTS assay Cytotoxic activity against human NCI-H929 cells after 72 hrs by MTS assay	[PMID: 24767818]
PC-3	IC₅₀	23.9 nM Compound: Carfilzomib	Antiproliferative activity against human PC3 cells after 72 hrs by MTS assay Antiproliferative activity against human PC3 cells after 72 hrs by MTS assay	[PMID: 30639896]
RKO	IC₅₀	27.1 nM Compound: Carfilzomib	Antiproliferative activity against human RKO cells after 72 hrs by oxyluciferin luminescence assay Antiproliferative activity against human RKO cells after 72 hrs by oxyluciferin luminescence assay	[PMID: 26231162]
RPMI-8226	IC₅₀	0.0067 μM Compound: Cfz	Cytotoxicity against human RPMI8226 cells after 48 hrs by MTT assay Cytotoxicity against human RPMI8226 cells after 48 hrs by MTT assay	[PMID: 30165344]
RPMI-8226	IC₅₀	0.007 μM Compound: Cfz	Cytotoxicity against human RPMI8226 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay Cytotoxicity against human RPMI8226 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay	[PMID: 30964987]
RPMI-8226	IC₅₀	13.19 nM Compound: Carfilzomib	Cytotoxic activity against human RPMI8226 cells after 72 hrs by MTS assay Cytotoxic activity against human RPMI8226 cells after 72 hrs by MTS assay	[PMID: 24767818]
RPMI-8226	IC₅₀	13.2 nM Compound: Carfilzomib	Cytotoxicity against human RPMI8226 cells measured after 72 hrs by MTS assay Cytotoxicity against human RPMI8226 cells measured after 72 hrs by MTS assay	[PMID: 28027531]
RPMI-8226	IC₅₀	13.2 nM Compound: Carfilzomib	Antiproliferative activity against human RPMI8226 cells measured after 72 hrs by MTS assay Antiproliferative activity against human RPMI8226 cells measured after 72 hrs by MTS assay	[PMID: 27765408]
RPMI-8226	IC₅₀	14.1 nM Compound: Carfilzomib	Antiproliferative activity against human RPMI-8226 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against human RPMI-8226 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 33223460]
RPMI-8226	IC₅₀	2 nM Compound: 2	Antiproliferative activity against human RPMI8226 cells after 72 hrs by MTS assay Antiproliferative activity against human RPMI8226 cells after 72 hrs by MTS assay	[PMID: 30611983]
RPMI-8226	IC₅₀	2.1 nM Compound: Carfilzomib	Antiproliferative activity against human RPMI8226 cells after 72 hrs by MTS assay Antiproliferative activity against human RPMI8226 cells after 72 hrs by MTS assay	[PMID: 30639896]
RPMI-8226	IC₅₀	39.1 nM Compound: Kyprolis(R)	Cytotoxicity against human RPMI8226 cells assessed as cell viability measured after 72 hrs by celltiter96 aqueous cell proliferation assay Cytotoxicity against human RPMI8226 cells assessed as cell viability measured after 72 hrs by celltiter96 aqueous cell proliferation assay	[PMID: 31383629]
TOV21G	IC₅₀	23.8 nM Compound: Carfilzomib	Antiproliferative activity against human TOV21G cells after 72 hrs by oxyluciferin luminescence assay Antiproliferative activity against human TOV21G cells after 72 hrs by oxyluciferin luminescence assay	[PMID: 26231162]
U-266	IC₅₀	35.7 nM Compound: Kyprolis(R)	Cytotoxicity against human U266B1 cells assessed as cell viability measured after 72 hrs by celltiter96 aqueous cell proliferation assay Cytotoxicity against human U266B1 cells assessed as cell viability measured after 72 hrs by celltiter96 aqueous cell proliferation assay	[PMID: 31383629]

In Vitro

Carfilzomib displays preferential in vitro inhibitory potency against the ChT-L activity in the β5 subunit, with over 80% inhibition at doses of 10 nM and above and little or no effect on the PGPH and T-L activities at doses up to 100 nM. Carfilzomib decreases the viability of ANBL-6, RPMI 8226 cells, U266 and KAS-6/1 cells with an IC₅₀ less than 5 nM. Carfilzomib overcome Dex resistance, in that MM1.R cells reveals an IC₅₀ of 15.2 nM, less than the value of 29.3 nM for parental MM1.S cells^[1]. Co-treatment with carfilzomib and HDACIs leads to synergistic induction of cell death in various mantle cell lymphoma lines and primary mantle cell lymphoma cells. Combined treatment with carfilzomib or ONX0912 with vorinostat in HF-4B and Granta cells sharply increases caspase activation, PARP cleavage, JNK activation, MnSOD2 induction, and DNA damage^[2].

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

In Vivo

Carfilzomib (2.0 mg/kg, i.v.) in conbination with 70 mg/kg vorinostat virtually abrogates tumor growth in Granta-luciferace cell xenograft flank model. Combined treatment results in a pronounced reduction in bioluminescence compared to animals treated with single agents or controls with minimal toxicity^[2].

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

Clinical Trial

Molecular Weight

719.91

Formula

C₄₀H₅₇N₅O₇

CAS No.

868540-17-4

Appearance

Solid

Color

White to off-white

SMILES

C[C@@]1(C([C@H](CC(C)C)NC([C@@H](NC([C@H](CC(C)C)NC([C@@H](NC(CN2CCOCC2)=O)CCC3=CC=CC=C3)=O)=O)CC4=CC=CC=C4)=O)=O)OC1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years

*The compound is unstable in solutions, freshly prepared is recommended.

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL (173.63 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	1.3891 mL	6.9453 mL	13.8906 mL
5 mM	0.2778 mL	1.3891 mL	2.7781 mL
10 mM	0.1389 mL	0.6945 mL	1.3891 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

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: 2.5 mg/mL (3.47 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (3.47 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 3

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: 2.5 mg/mL (3.47 mM); Suspended solution; Need ultrasonic

Purity & Documentation

Purity: 99.98%

Data Sheet (280 KB) SDS (393 KB)

COA (251 KB) HNMR (298 KB) RP-HPLC (242 KB) LCMS (87 KB)

Handling Instructions (2659 KB)

References

[1]. Kuhn DJ, et al. Potent activity of carfilzomib, a novel, irreversible inhibitor of the ubiquitin-proteasome pathway, against preclinical models of multiple myeloma. Blood. 2007 Nov 1;110(9):3281-90. [Content Brief]

[2]. Dasmahapatra G, et al. Carfilzomib interacts synergistically with histone deacetylase inhibitors in mantle cell lymphoma cells in vitro and in vivo. Mol Cancer Ther. 2011 Sep;10(9):1686-97. [Content Brief]

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