Vemurafenib (Synonyms: 维罗非尼; PLX4032; RG7204; RO5185426)

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Data Sheet SDS COA 产品使用指南

摩尔计算器

Vemurafenib (PLX4032; RG7204; RO5185426) 是首创的，有效的 B-RAF 选择性抑制剂，能够抑制 RAF^V600E 和 c-RAF-1 的活性，IC₅₀ 分别为 31 nM 和 48 nM。Vemurafenib 可以诱导细胞自噬 (autophagy)。

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Vemurafenib Chemical Structure

CAS No. : 918504-65-1

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥567	In-stock
5 mg	￥321	In-stock
10 mg	￥515	In-stock
50 mg	￥1450	In-stock
100 mg	￥2320	In-stock
500 mg	现货	询价
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5 g		询价

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Customer Review

Other Forms of Vemurafenib:

MCE 顾客使用本产品发表的 75 篇科研文献

: Vemurafenib purchased from MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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.

: Vemurafenib purchased from MCE. 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 MCE. 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 MCE. 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.

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BRaf c-Raf Raf

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

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)

细胞效力
(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]

体外研究
(In Vitro)

Vemurafenib (PLX4032) 选择性阻断 BRAF 突变细胞中的 RAF/MEK/ERK 通路^[1]。Vemurafenib 是 17 种黑色素瘤细胞系中表达 RAF^V600E 但不表达 BRAF^WT 的细胞的强效增殖抑制剂。Vemurafenib 在 CHL-1 细胞中以高浓度诱导 MEK 和 ERK 磷酸化^[2]。黑色素瘤细胞中 EGFR 的异位表达足以导致对 Vemurafenib 的耐药性^[3]。

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

体内研究
(In Vivo)

Vemurafenib (PLX4032，20、25、75 mg/kg，口服) 可引起剂量依赖性肿瘤生长抑制，较高剂量可导致 BRAF 突变异种移植瘤的肿瘤消退^[1]。Vemurafenib (12.5、25 和 75 mg/kg，口服) 可显著抑制肿瘤生长，并诱导携带 LOX 肿瘤异种移植瘤的小鼠的肿瘤消退^[2]。

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

Clinical Trial

分子量

489.92

Formula

C₂₃H₁₈ClF₂N₃O₃S

CAS 号

918504-65-1

性状

固体

颜色

White to gray

中文名称

维罗非尼；维罗菲尼；威罗菲尼；唯罗非尼

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

溶解性数据

细胞实验：

DMSO 中的溶解度 : 50 mg/mL (102.06 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	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

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

摩尔计算器
稀释计算器

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.25 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.25 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

方案一

请依序添加每种溶剂： 1.5% CMC-Na/saline water
Solubility: 3.33 mg/mL (6.80 mM); 悬浊液; 超声助溶

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.85%

选择批次：

Data Sheet (641 KB) SDS (393 KB)

COA (287 KB) HNMR (280 KB) RP-HPLC (198 KB) LCMS (94 KB)

产品使用指南 (1538 KB)

参考文献

[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.
参考文献	[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]

Vemurafenib 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	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

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Vemurafenib (Synonyms: 维罗非尼; PLX4032; RG7204; RO5185426)

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Vemurafenib (Synonyms: 维罗非尼; PLX4032; RG7204; RO5185426)

Customer Review

Other Forms of Vemurafenib:

Vemurafenib 相关抗体

MCE 顾客使用本产品发表的 75 篇科研文献

Vemurafenib 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Raf 亚型特异性产品:

生物活性

实验参考方法

纯度 & 产品资料

参考文献

Vemurafenib 相关抗体:

摩尔计算器

稀释计算器

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完整储备液配制表

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