Cat. No.: HY-12057

Vemurafenib

(Synonyms: PLX4032; RG7204; RO5185426)

104 Cited Publications

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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. Vemurafenib induces cell autophagy.

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Pureté: 99.90%
CAS No.: 918504-65-1
Formule: C₂₃H₁₈ClF₂N₃O₃S
Masse moléculaire:489.92

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Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Vemurafenib Chemical Structure

CAS No.: 918504-65-1

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (104)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
Pureté et documentation
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Activité biologique

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)

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Cellular Effect

Cell Line	Type	Value	Description	References
8505C	IC₅₀	2.94 μM Compound: 1; Vem	Cytotoxicity against human 8505C cells expressing homozygous BRAF V600E mutant assessed as cell growth measured after 7 days of treatment by crystal violet assay Cytotoxicity against human 8505C cells expressing homozygous BRAF V600E mutant assessed as cell growth measured after 7 days of treatment by crystal violet assay	[PMID: 37182332]
A2058	IC₅₀	8.7 μM Compound: Vemurafenib	Cytotoxicity against human A2058 cells Cytotoxicity against human A2058 cells	[PMID: 32631547]
A-375	IC₅₀	0.31 μM Compound: 2, PLX4032	Antiproliferative activity against human A375 cells expressing B-Raf V600E mutant and wild type Ras Antiproliferative activity against human A375 cells expressing B-Raf V600E mutant and wild type Ras	[PMID: 22808911]
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	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	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	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	0.102 μM Compound: Chemical probe : Vemurafenib	Antiproliferative activity against human A-375 cells harboring BRAF V600E mutation assessed as reduction in cell viability incubated for 72 hrs by CellTitre-Glo assay Antiproliferative activity against human A-375 cells harboring BRAF V600E mutation assessed as reduction in cell viability incubated for 72 hrs by CellTitre-Glo assay	[PMID: 25915038]
A-375	IC₅₀	5.476 μM Compound: Chemical probe : Vemurafenib	Antiproliferative activity against human vemurafenib-resistant A-375 cells harboring BRAF V600E mutation assessed as reduction in cell viability incubated for 72 hrs by CellTitre-Glo assay Antiproliferative activity against human vemurafenib-resistant A-375 cells harboring BRAF V600E mutation assessed as reduction in cell viability incubated for 72 hrs by CellTitre-Glo assay	[PMID: 25915038]
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	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	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]
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	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	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	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	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	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	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	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	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	0.09 μM Compound: 1	Cytotoxicity against human A-375 cells incubated for 96 hrs by MTT assay Cytotoxicity against human A-375 cells incubated for 96 hrs by MTT assay	[PMID: 36878151]
C32	IC₅₀	0.084 μM Compound: 1; Vem	Cytotoxicity against human C32 cells expressing heterozygous BRAF V600E mutant assessed as cell growth measured after 7 days of treatment by crystal violet assay Cytotoxicity against human C32 cells expressing heterozygous BRAF V600E mutant assessed as cell growth measured after 7 days of treatment by crystal violet assay	[PMID: 37182332]
CHL-1	IC₅₀	>10 μM Compound: Chemical probe : Vemurafenib	Antiproliferative activity against human CHL-1 cells assessed as reduction in cell viability incubated for 72 hrs by CellTitre-Glo assay Antiproliferative activity against human CHL-1 cells assessed as reduction in cell viability incubated for 72 hrs by CellTitre-Glo assay	[PMID: 25915038]
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	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]
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]
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	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	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	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	>2 μM Compound: 2, PLX4032	Antiproliferative activity against human HCT116 cells expressing wild type b-Raf and KRAS mutant Antiproliferative activity against human HCT116 cells expressing wild type b-Raf and KRAS mutant	[PMID: 22808911]
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	>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	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	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	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	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	0.601 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	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	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	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]
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	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	0.049 μM Compound: 1; Vem	Cytotoxicity against human HT-29 cells expressing heterozygous BRAF V600E mutant assessed as cell growth measured after 7 days of treatment by crystal violet assay Cytotoxicity against human HT-29 cells expressing heterozygous BRAF V600E mutant assessed as cell growth measured after 7 days of treatment by crystal violet assay	[PMID: 37182332]
L929	EC₅₀	3.75 μM Compound: F12	Anti-necroptosis activity against TNFalpha-induced mouse L929 cells assessed as reduction in cell viability Anti-necroptosis activity against TNFalpha-induced mouse L929 cells assessed as reduction in cell viability	[PMID: 38199165]
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]
M14	IC₅₀	150 nM Compound: Zelboraf, RG7204, PLX4032, RO5185426	Cytotoxicity against human M14 cells expressing NRAS G12C mutant Cytotoxicity against human M14 cells expressing NRAS G12C mutant	[PMID: 24471466]
M14	IC₅₀	0.088 μM Compound: Chemical probe : Vemurafenib	Antiproliferative activity against human M14 cells harboring BRAF V600E mutation assessed as reduction in cell viability incubated for 72 hrs by CellTitre-Glo assay Antiproliferative activity against human M14 cells harboring BRAF V600E mutation assessed as reduction in cell viability incubated for 72 hrs by CellTitre-Glo assay	[PMID: 25915038]
M14	IC₅₀	3.856 μM Compound: Chemical probe : Vemurafenib	Antiproliferative activity against human vemurafenib-resistant M14 cells harboring BRAF V600E mutation assessed as reduction in cell viability incubated for 72 hrs by CellTitre-Glo assay Antiproliferative activity against human vemurafenib-resistant M14 cells harboring BRAF V600E mutation assessed as reduction in cell viability incubated for 72 hrs by CellTitre-Glo assay	[PMID: 25915038]
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: Chemical probe : Vemurafenib	Antiproliferative activity against human SK-MEL-2 cells harboring NRAS Q61R mutation assessed as reduction in cell viability incubated for 72 hrs by CellTitre-Glo assay Antiproliferative activity against human SK-MEL-2 cells harboring NRAS Q61R mutation assessed as reduction in cell viability incubated for 72 hrs by CellTitre-Glo assay	[PMID: 25915038]
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	5.64 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-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-28	IC₅₀	0.1 μM Compound: Zelboraf, RG7204, PLX4032, RO5185426	Cytotoxicity against human SK-MEL-28 cells expressing B-raf V600E mutant Cytotoxicity against human SK-MEL-28 cells expressing B-raf V600E mutant	[PMID: 24471466]
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]
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]
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	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	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 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.

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.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 918504-65-1
Appearance Solid
Masse moléculaire 489.92
Formule C₂₃H₁₈ClF₂N₃O₃S
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
Synonyms

PLX4032; RG7204; RO5185426
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (104)

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Cancer Cell

Integrated proteogenomic characterization of glioblastoma evolution. [Abstract]

2024 Mar 11;42(3):358-377.e8. PMID: 38215747
Cell Metab

Realigned transsulfuration drives BRAF-V600E-targeted therapy resistance in melanoma. [Abstract]

2025 May 6;37(5):1171-1188.e9. PMID: 40037361
Nat Cancer

The GENEVA platform models tumor mosaicism to reveal variations of responses to KRAS inhibitors and identify improved drug combinations. [Abstract]

2026 Feb 24. PMID: 41735640
Nat Biomed Eng

TLR7/8-agonist-loaded nanoparticles promote the polarization of tumour-associated macrophages to enhance cancer immunotherapy. [Abstract]

2018 Aug;2(8):578-588. PMID: 31015631
Cell Res

Three-dimensional bioprinted glioblastoma microenvironments model cellular dependencies and immune interactions. [Abstract]

2020 Oct;30(10):833-853. PMID: 32499560
Cell Host Microbe

Peptostreptococcus stomatis promotes colonic tumorigenesis and receptor tyrosine kinase inhibitor resistance by activating ERBB2-MAPK. [Abstract]

2024 Jul 23:S1931-3128(24)00254-3. PMID: 39059397
Nat Commun

Synthetic vectors for activating the driving axis of ferroptosis. [Abstract]

2024 Sep 10;15(1):7923. PMID: 39256387
Nat Commun

Highly multiplexed imaging of single cells using a high-throughput cyclic immunofluorescence method. [Abstract]

2015 Sep 24;6:8390. PMID: 26399630
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
J Extracell Vesicles

TMTP1-Modified Small Extracellular Vesicles Target BRAF Mutation in Anaplastic Thyroid Cancer Reversing Vemurafenib Resistance With CRISPR/Cas9 Delivery. [Abstract]

2025 Sep;14(9):e70170. PMID: 41002137
Adv Sci (Weinh)

Lactylation of HDAC1 Confers Resistance to Ferroptosis in Colorectal Cancer. [Abstract]

2025 Jan 31:e2408845. PMID: 39888307
Adv Sci (Weinh)

Patient-Derived Melanoma Immune-Tumoroids as a Platform for Precise High throughput Drug Screening. [Abstract]

2024 Dec;11(48):e2408707. PMID: 39475010
Cell Discov

Lineage-coupled clonal capture identifies clonal evolution mechanisms and vulnerabilities of BRAFV600E inhibition resistance in melanoma. [Abstract]

2022 Oct 6;8(1):102. PMID: 36202798
Sci Adv

BRAF inhibitors promote intermediate BRAF(V600E) conformations and binary interactions with activated RAS. [Abstract]

2019 Aug 14;5(8):eaav8463. PMID: 31453322
EBioMedicine

EGFR/uPAR interaction as druggable target to overcome vemurafenib acquired resistance in melanoma cells. [Abstract]

2019 Jan:39:194-206. PMID: 30611716

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.
Cell Rep Med

CAN-Scan: A multi-omic phenotype-driven precision oncology platform identifies prognostic biomarkers of therapy response for colorectal cancer. [Abstract]

2025 Apr 2:102053. PMID: 40187357
Clin Cancer Res

The activation of MAPK in melanoma cells resistant to BRAF inhibition promotes PD-L1 expression that is reversible by MEK and PI3K inhibition. [Abstract]

2013 Feb 1;19(3):598-609. PMID: 23095323

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.
Cancer Lett

Everolimus selectively targets vemurafenib resistant BRAFV600E melanoma cells adapted to low pH. [Abstract]

2017 Nov 1:408:43-54. PMID: 28826720

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.
Cell Death Dis

Fyn inhibition by TAE684: A synergistic strategy to suppress melanoma and reverse vemurafenib resistance. [Abstract]

2025 Nov 6;16(1):796. PMID: 41198656
Cell Death Dis

Exploiting mitochondrial dysfunction to overcome BRAF inhibitor resistance in advanced melanoma: the role of disulfiram as a copper ionophore. [Abstract]

2025 Jul 1;16(1):482. PMID: 40592836
Cell Death Dis

Triggering of endoplasmic reticulum stress via ATF4-SPHK1 signaling promotes glioblastoma invasion and chemoresistance. [Abstract]

2024 Aug 1;15(8):552. PMID: 39090107
Adv Healthc Mater

Biofabrication and Monitoring of a 3D Printed Skin Model for Melanoma. [Abstract]

2024 Jul 11:e2401136. PMID: 38992996
Cell Death Dis

POU4F1 promotes the resistance of melanoma to BRAF inhibitors through MEK/ERK pathway activation and MITF up-regulation. [Abstract]

2020 Jun 12;11(6):451. PMID: 32532957
Proc Natl Acad Sci U S A

LINEAGE: Label-free identification of endogenous informative single-cell mitochondrial RNA mutation for lineage analysis. [Abstract]

2022 Feb 1;119(5):e2119767119. PMID: 35086932
Proc Natl Acad Sci U S A

Mutation-oriented profiling of autoinhibitory kinase conformations predicts RAF inhibitor efficacies. [Abstract]

2020 Dec 8;117(49):31105-31113. PMID: 33229534
Acta Pharmacol Sin

Osimertinib successfully combats EGFR-negative glioblastoma cells by inhibiting the MAPK pathway. [Abstract]

2021 Jan;42(1):108-114. PMID: 32398685
Phytomedicine

Parthenolide inhibits Hsp90α ATPase activity and overcomes acquired BRAF-inhibitor resistance in cutaneous melanoma. [Abstract]

2025 Oct:146:157151. PMID: 40815947
ACS Appl Mater Interfaces

A New Spin on Antibody-Drug Conjugates: Trastuzumab-Fulvestrant Colloidal Drug Aggregates Target HER2-Positive Cells. [Abstract]

2017 Apr 12;9(14):12195-12202. PMID: 28319364
NPJ Precis Oncol

PERK mediates resistance to BRAF inhibition in melanoma with impaired PTEN. [Abstract]

2021 Jul 19;5(1):68. PMID: 34282258
Neoplasia

A methyl-to-acetyl switch in H3K27 drives metabolic reprogramming and resistance to BRAFV600E inhibition in melanoma. [Abstract]

2025 Oct:68:101223. PMID: 40850308
Cell Syst

Resistor: An algorithm for predicting resistance mutations via Pareto optimization over multistate protein design and mutational signatures. [Abstract]

2022 Oct 19;13(10):830-843.e3. PMID: 36265469
Cell Syst

Receptor-Driven ERK Pulses Reconfigure MAPK Signaling and Enable Persistence of Drug-Adapted BRAF-Mutant Melanoma Cells. [Abstract]

2020 Nov 18;11(5):478-494.e9. PMID: 33113355
Cell Syst

A Library of Phosphoproteomic and Chromatin Signatures for Characterizing Cellular Responses to Drug Perturbations. [Abstract]

2018 Apr 25;6(4):424-443.e7. PMID: 29655704
Mol Syst Biol

Adaptive resistance of melanoma cells to RAF inhibition via reversible induction of a slowly dividing de-differentiated state. [Abstract]

2017 Jan; 13(1): 905. PMID: 28069687

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

Western blotting for NGFR-inducible COLO858 cells, NGFR^High A375 and WM115 cells, and NGFR^Low MACSF and MZ7MEL cells, treated for 48 h with 0.2 or 1 μM Vmurafenib or DMSO.
Mol Syst Biol

Systematic analysis of BRAF(V600E) melanomas reveals a role for JNK/c-Jun pathway in adaptive resistance to drug-induced apoptosis. [Abstract]

2015 Mar 26;11(3):797. PMID: 25814555
NPJ Breast Cancer

SIMD: Synergistic integration mutualistic platform based on single-cell and proteotranscriptomics for drug repositioning. [Abstract]

2025 Dec 24;12(1):4. PMID: 41444222
Biomed Pharmacother

High levels of soluble CD73 unveil resistance to BRAF inhibitors in melanoma cells. [Abstract]

2024 Jun 27:177:117033. PMID: 38941889
Oncogene

The dimer-dependent catalytic activity of RAF family kinases is revealed through characterizing their oncogenic mutants. [Abstract]

2018 Oct;37(43):5719-5734. PMID: 29930381

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.
PLoS Biol

The cell cycle regulator PLK1 promotes murine melanoma progression by regulating the transcription factor BACH1. [Abstract]

2025 Nov 24;23(11):e3003490. PMID: 41284701
Cell Rep

Kinetics of RTK activation determine ERK reactivation and resistance to dual BRAF/MEK inhibition in melanoma. [Abstract]

2023 May 29;42(6):112570. PMID: 37252843
Cell Rep

Reprogramming of bivalent chromatin states in NRAS mutant melanoma suggests PRC2 inhibition as a therapeutic strategy. [Abstract]

2021 Jul 20;36(3):109410. PMID: 34289358
Anal Chem

Precise Readout of MEK1 Proteoforms upon MAPK Pathway Modulation by Individual Ion Mass Spectrometry. [Abstract]

2024 Mar 19;96(11):4455-4462. PMID: 38458998
Elife

RNF43 inhibits WNT5A-driven signaling and suppresses melanoma invasion and resistance to the targeted therapy. [Abstract]

2021 Oct 27;10:e65759. PMID: 34702444
Cancer Cell Int

Construction of a prognostic model with histone modification-related genes and identification of potential drugs in pancreatic cancer. [Abstract]

2021 Jun 5;21(1):291. PMID: 34090418
Cell Biol Toxicol

Neddylation signaling inactivation by tetracaine hydrochloride suppresses cell proliferation and alleviates vemurafenib-resistance of melanoma. [Abstract]

2024 Sep 19;40(1):81. PMID: 39297891
J Invest Dermatol

Vemurafenib Drives Epithelial-to-Mesenchymal Transition Gene Expression in BRAF Inhibitor‒Resistant BRAFV600E/NRASQ61K Melanoma Enhancing Tumor Growth and Metastasis in a Bioluminescent Murine Model. [Abstract]

2022 May;142(5):1456-1465.e1. PMID: 34687745
Biochem Pharmacol

Phospholipase D2 regulation by transcription factor FOXA1 promotes the drug resistance of vemurafenib in melanoma cells. [Abstract]

2025 Dec;242(Pt 4):117434. PMID: 41110487
Pharmaceutics

Drug Repurposing for the Identification of Compounds with Anti-SARS-CoV-2 Capability via Multiple Targets. [Abstract]

2022 Jan 12;14(1):176. PMID: 35057070
J Enzyme Inhib Med Chem

The Carbonic Anhydrase IX inhibitor SLC-0111 as emerging agent against the mesenchymal stem cell-derived pro-survival effects on melanoma cells. [Abstract]

2020 Dec;35(1):1185-1193. PMID: 32396749
Life Sci

Identification of UBE3C as an E3 ubiquitin ligase for mutant BRAF. [Abstract]

2025 Oct 1:378:123827. PMID: 40602747
Inflammation

ZAKα Induces Pyroptosis of Colonic Epithelium Via the Caspase-11/GSDMD Pathway to Aggravate Colitis. [Abstract]

2025 Feb 24. PMID: 39992609
Nutrients

Oleuropein, the Main Polyphenol of Olea europaea Leaf Extract, Has an Anti-Cancer Effect on Human BRAF Melanoma Cells and Potentiates the Cytotoxicity of Current Chemotherapies. [Abstract]

2018 Dec 8;10(12). pii: E1950. PMID: 30544808

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.
Int J Mol Sci

Hydroxytyrosol Reprograms the Tumor Microenvironment in 3D Melanoma Models by Suppressing ERBB Family and Kinase Pathways. [Abstract]

2025 Jul 20;26(14):6957. PMID: 40725203
Int J Mol Sci

Neutrophil Extracellular Trap Formation Model Induced by Monosodium Urate and Phorbol Myristate Acetate: Involvement in MAPK Signaling Pathways. [Abstract]

2024 Dec 27;26(1):143. PMID: 39796001
Int J Mol Sci

Suppressing Effect of Na+/Ca2+ Exchanger (NCX) Inhibitors on the Growth of Melanoma Cells. [Abstract]

2022 Jan 14;23(2):901. PMID: 35055084
Int J Oncol

Epigenetic inhibitors eliminate senescent melanoma BRAFV600E cells that survive long‑term BRAF inhibition. [Abstract]

2020 Jun;56(6):1429-1441. PMID: 32236593
Pharmaceuticals (Basel)

Design, Synthesis, and Bioactivity Assessment of Modified Vemurafenib Analog. [Abstract]

2025 Aug 5;18(8):1161. PMID: 40872552
Int Immunopharmacol

Keratinocyte-derived exosomal miR-31-5p reduces vemurafenib sensitivity in melanoma cells. [Abstract]

2026 Jun 15:179:116659. PMID: 41997057
ACS Appl Bio Mater

Decellularized Dermis ECM-Based Melanoma-on-a-Chip Model with Integrated Lymphatic and Vascular Networks for High-Throughput Drug Testing. [Abstract]

2026 Feb 18. PMID: 41708064
Int J Cancer

BRAFV600E mutation: A promising target in colorectal neuroendocrine carcinoma. [Abstract]

2019 Mar 15;144(6):1379-1390. PMID: 30144031

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.
Mol Pharm

Molecular Interactions of Cobimetinib and Vemurafenib with Human Serum Albumin: a Comparative Biophysical and Computational Analysis. [Abstract]

2025 Aug 4;22(8):4969-4982. PMID: 40662409
Cell Rep Methods

RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]

2023 Oct 23;3(10):100599. PMID: 37797618
BMC Biol

Efficient prioritization of CRISPR screen hits by accounting for targeting efficiency of guide RNA. [Abstract]

2023 Feb 24;21(1):45. PMID: 36829149
Cancers (Basel)

In Vitro and In Vivo Drug-Response Profiling Using Patient-Derived High-Grade Glioma. [Abstract]

2023 Jun 22;15(13):3289. PMID: 37444398
Front Cell Dev Biol

Fast Dynamic in vivo Monitoring of Erk Activity at Single Cell Resolution in DREKA Zebrafish. [Abstract]

2018 Sep 25:6:111. PMID: 30320107
J Mol Med (Berl)

Roles of different IRES-dependent FGF2 isoforms in the acquisition of the major aggressive features of human metastatic melanoma. [Abstract]

2017 Jan;95(1):97-108. PMID: 27558498

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).
Oncol Res

CEP55 Promotes Acral Melanoma Progression via MAPK Pathway and Predicts Survival Following Immunotherapy. [Abstract]

2025 Aug 28;33(9):2507-2527. PMID: 40918457
Sci Rep

The unexplored mechanism of antitumoral effect of pirfenidone in melanoma cells. [Abstract]

2025 Aug 1;15(1):28071. PMID: 40751072
Oncol Rep

Icariside II overcomes BRAF inhibitor resistance in melanoma by inducing ROS production and inhibiting MITF. [Abstract]

2020 Jul;44(1):360-370. PMID: 32319656
Sci Rep

Tissue-engineered 3D melanoma model with blood and lymphatic capillaries for drug development. [Abstract]

2018 Sep 4;8(1):13191. PMID: 30181613
Oncol Rep

Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues. [Abstract]

2018 Aug;40(2):635-646. PMID: 29917168
ACS Chem Biol

Stable Colloidal Drug Aggregates Catch and Release Active Enzymes. [Abstract]

2016 Apr 15;11(4):992-1000. PMID: 26741163
Bioengineering (Basel)

Precision Oncology for High-Grade Gliomas: A Tumor Organoid Model for Adjuvant Treatment Selection. [Abstract]

2025 Oct 19;12(10):1121. PMID: 41155119
Biology (Basel)

Secretome Screening of BRAFV600E-Mutated Colon Cancer Cells Resistant to Vemurafenib. [Abstract]

2023 Apr 17;12(4):608. PMID: 37106808
Viruses

Identification and Tracking of Antiviral Drug Combinations. [Abstract]

2020 Oct 18;12(10):1178. PMID: 33080984
Exp Cell Res

Network-based analysis with primary cells reveals drug response landscape of acute myeloid leukemia. [Abstract]

2020 Aug 1;393(1):112054. PMID: 32376287
Dis Model Mech

Vemurafenib partially ameliorates muscle histopathology but does not improve muscle function in a mouse model of LAMA2-CMD. [Abstract]

2023 Jun 1;16(6):dmm049916. PMID: 37021539
Mol Inform

In Silico Identification of Novel and Potent Inhibitors Against Mutant BRAF (V600E), MD Simulations, Free Energy Calculations, and Experimental Determination of Binding Affinity. [Abstract]

2025 Jun;44(5-6):e2400372. PMID: 40524540
Cell Biol Int

Sensitization of HT29 colorectal cancer cells to vemurafenib in three-dimensional collagen cultures. [Abstract]

2020 Feb;44(2):621-629. PMID: 31736196
Mol Pharmacol

Influence of Tyrosine Kinase Inhibition on Organic Anion Transporting Polypeptide 1B3-Mediated Uptake. [Abstract]

2022 Jun;101(6):381-389. PMID: 35383108
Life Sci Alliance

LuminoCell: a versatile and affordable platform for real-time monitoring of luciferase-based reporters. [Abstract]

2022 Apr 19;5(8):e202201421. PMID: 35440493
PLoS One

A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]

2024 Nov 1;19(11):e0308647. PMID: 39485774
Clin Exp Pharmacol Physiol

Diclofenac Enhances the Response of BRAF Inhibitor to Melanoma Through ROS/p38/p53 Signaling. [Abstract]

2025 Mar;52(3):e70022. PMID: 39788129
Fundam Clin Pharmacol

Inhibition of organic cation transporter 3 activity by tyrosine kinase inhibitors. [Abstract]

2021 Oct;35(5):919-929. PMID: 33523504
Eur J Drug Metab Pharmacokinet

Differential Inhibition of Equilibrative Nucleoside Transporter 1 (ENT1) Activity by Tyrosine Kinase Inhibitors. [Abstract]

2021 Sep;46(5):625-635. PMID: 34275128
Radiol Oncol

Electrochemotherapy with bleomycin is effective in BRAF mutated melanoma cells and interacts with BRAF inhibitors. [Abstract]

2016 Jul 19;50(3):274-9. PMID: 27679543
Arch Dermatol Res

EGFR influences the resistance to targeted therapy in BRAF V600E melanomas by regulating the ferroptosis process. [Abstract]

2025 Mar 1;317(1):514. PMID: 40024937
Res Sq

2026 Feb 18.
SSRN

2025 Nov 14.
Appl Biosci (Basel)
University of Minnesota

2024.
Preprints

2024 Apr 26.
bioRxiv

Inferring therapeutic vulnerability within tumors through integration of pan-cancer cell line and single-cell transcriptomic profiles. [Abstract]

2023 Nov 1:2023.10.29.564598. PMID: 37961545
Norwegian University of Science and Technology

2023 May.
bioRxiv

2023 Jan 17.
Research Square Print

December 21st, 2022.
SSRN

2022 Nov 21.
Preprints

2022, 2022070375.
J Pers Med

Enrichment of SOX2-Positive Cells in BRAF V600E Mutated and Recurrent Ameloblastoma. [Abstract]

2022 Jan 8;12(1):77. PMID: 35055392
Norwegian University of Science and Technology

2021 Oct.
Research Square Preprint

2021 May.
bioRxiv

2020 Feb 10.
bioRxiv

2019 Sep.
University of Toronto

2019 Aug.

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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.

Working 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: 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:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

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%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
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%
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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).

Working solution concentration: 0.22 mg/mL

Protocole

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.

MedChemExpress (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).

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (279 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
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OR (2659 KB)
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SEC-HPLC (2659 KB)
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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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Vemurafenib

104 Cited Publications

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Vemurafenib

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