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Vemurafenib [918504-65-1]

Imprimer

Référence HY-12057-50mg

Conditionnement : 50mg

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Description

Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC₅₀s of 31 and 48 nM for RAF^V600E and c-RAF-1, respectively^[1]^[4]. Vemurafenib induces cell autophagy^[5].

IC₅₀ & Target^[1]

B-Raf^V600E

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 RAF^V600E but not BRAF^WT 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.

Solvant et solubilité

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
10 mM	0.2041 mL	1.0206 mL	2.0411 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.

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

Pureté et documentation

Purity: 99.85%

Fiche technique (279 KB) SDS (393 KB)

COA (249 KB) HNMR (280 KB) RP-HPLC (198 KB) LCMS (94 KB)

Instruction de manipulation (2659 KB)

Références

[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]

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Vemurafenib [918504-65-1]

Référence HY-12057-50mg

Contactez votre distributeur local :

Marque : MedChemExpress

Contactez votre distributeur local :

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