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Vemurafenib/维罗非尼 {[allProObj[0].p_purity_real_show]}

货号：A116840 同义名： PLX4032; RG7204

Vemurafenib（PLX4032）是一种首创、选择性且强效的B-RAF激酶抑制剂，对RAFV600E和c-RAF-1的IC50分别为31 nM和48 nM。Vemurafenib诱导细胞自噬。

Vemurafenib/维罗非尼 化学结构 CAS号：918504-65-1
Vemurafenib/维罗非尼 化学结构
CAS号：918504-65-1
Vemurafenib/维罗非尼 3D分子结构
CAS号：918504-65-1
Vemurafenib/维罗非尼 化学结构 CAS号：918504-65-1
Vemurafenib/维罗非尼 3D分子结构 CAS号：918504-65-1
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Vemurafenib/维罗非尼 纯度/质量文件 产品仅供科研

货号：A116840 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
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• Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]
• Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]
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产品名称 A-raf ↓ B-Raf ↓ C-Raf/Raf-1 ↓ Raf ↓ 其他靶点 纯度
Encorafenib ✔ 99%+
GDC-0879 ++++

B-Raf, IC50: 0.13 nM

 		99%+
SB-590885 ++++

B-Raf, Ki: 0.16 nM

 		99%+
RAF265 99%+
Dabrafenib ++++

B-Raf, IC50: 5.2 nM

B-Raf (V600E), IC50: 0.7 nM

 		+++

C-Raf, IC50: 6.3 nM

 		98%
Lifirafenib ++++

WT A-RAF, IC50: 1 nM

 		++

BRAF WT, IC50: 32 nM

BRAF(V600E), IC50: 23 nM

 		+++

C-RAF (Y340/341D), IC50: 7 nM

 		EGFR 98%
ZM 336372 +

C-Raf, IC50: 70 nM

 		99%+
NVP-BHG 712 +

C-Raf, IC50: 0.395 μM

 		99%+
CCT196969 +

BRAF, IC50: 0.1 μM

 		++

CRAF, IC50: 0.01 μM

 		Src 98%
Vemurafenib ++

B-Raf, IC50: 100 nM

B-Raf (V600E), IC50: 31 nM

 		+

C-Raf, IC50: 48 nM

 		98+%
PLX4720 ++

B-Raf, IC50: 160 nM

B-Raf (V600E), IC50: 13 nM

 		+++

C-Raf-1 (Y340D/Y341D), IC50: 6.7 nM

 		BRK 99+%
GW 5074 +++

C-Raf, IC50: 9 nM

 		99%+
Avutometinib +++

BRAF, IC50: 19 nM

BRAF V600E, IC50: 8.2 nM

 		+

CRAF, IC50: 56 nM

 		98%
LY3009120 ++++

BRAF WT, IC50: 15 nM

BRAF(V600E), IC50: 5.8 nM

 		++++

C-Raf, IC50: 4.3 nM

 		99%+
Agerafenib ++

B-Raf, Kd: 36 nM

B-Raf (V600E), Kd: 14 nM

 		+

C-Raf, Kd: 39 nM

 		RET 99%+
TAK-632 +++

B-Raf, IC50: 8.3 nM

 		++++

C-Raf, IC50: 1.4 nM

 		99%+
AZ 628 +

B-Raf, IC50: 105 nM

B-Raf (V600E), IC50: 34 nM

 		++

C-Raf-1, IC50: 29 nM

 		98%
PLX7904 ✔ 98+%
Sorafenib ++

B-Raf, IC50: 22 nM

B-Raf (V599E), IC50: 38 nM

 		++++

Raf-1, IC50: 6 nM

 		++++

Raf-1, IC50: 6 nM

 		99%
Tovorafenib ✔ 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Vemurafenib/维罗非尼 生物活性

靶点

  • B-Raf

    B-Raf, IC50:100 nM

    B-Raf (V600E), IC50:31 nM

  • C-Raf/Raf-1

    C-Raf, IC50:48 nM
描述 The RAS/RAF signaling pathway is an important mediator of tumor cell proliferation and angiogenesis. Among them, B-RAF is the most frequently mutated protein kinase in human cancers. Vemurafenib is a selective inhibitor of B-RafV600E mutant with IC50 value of 31nM (measured by enzymatic activity) displays similar potency c-RAF-1 (IC50=48nM), selective against many other kinases, including wild-type B-RAF (IC50=100nM)[1]. Vemurafenib potently and selectively inhibited proliferation in those melanoma cell lines expressing B-RafV600E mutant but not BRAF-WT. Vemurafenib can inhibit p-MEK and p-ERK in B-RafV600E- expressing melanoma cell lines, Colo829 and LOX (>0.24μM, for 2h), as well as in WM2664 and WM1341D cell lines (>0.24μM, for 2h), which expresses BRAFV600D and BRAFV600R, respectively. However, Vemurafenib showed more variable effect on p-MEK and p-ERK of cell lines that do not express codon 600 BRAF mutations, such as CHL-1 (BRAFWT) and SK-MEL2 (BRAFWT), and HMVII (BRAFG469V) cell line. Vemurafenib possessed good pharmacodynamics as an association between plasma concentration and inhibition of p-MEK and p-ERK can be observed, with the highest plasma concentration (124 μmol/L at 2h) corresponding to the highest mean percent inhibition of phosphorylation (70.5% for MEK and 52% for ERK)[2]. Oral gavage with Vemurafenib (6/20mg/kg, QD, or 20mg/kg, BID) demonstrated dose-dependent inhibition of tumour growth, with higher exposures (25/75mg/kg, BID) resulting in tumour regression, in COLO205 B-RafV600E mutant xenografts[1].
作用机制 Vemurafenib is an ATP-competitive inhibitor of mutant BRAF.[1]

Vemurafenib/维罗非尼 细胞实验

Cell Line
Concentration Treated Time Description References
MEL-XY3 10 µM 5 weeks To study the effects of long-term PLX4032 treatment on BRAFV600E-mutated melanoma cell lines. The majority of melanoma cells died, but a proportion of cells remained viable and quiescent, presenting senescent cancer stem cell-like characteristics. Int J Oncol. 2020 Jun;56(6):1429-1441.
A375-R cells 2.5 µM 5 days Assessed the inhibitory effect of Vemurafenib on resistant cell proliferation, showing that A375-R cells were insensitive to Vemurafenib. Sci Rep. 2019 Oct 2;9(1):14197
A375-P cells 0.1 µM 5 days Assessed the inhibitory effect of Vemurafenib on cell proliferation, showing that 0.1 µM Vemurafenib was sufficient to inhibit 50% of cell proliferation. Sci Rep. 2019 Oct 2;9(1):14197
SK-Mel-19R 2 μM 2 months To select vemurafenib-resistant melanoma cell lines and analyze the activation of the RhoA signaling pathway. Oncogene. 2020 Feb;39(7):1466-1483.
UACC62R 2 μM 2 months To select vemurafenib-resistant melanoma cell lines and analyze the activation of the RhoA signaling pathway. Oncogene. 2020 Feb;39(7):1466-1483.
K-1 10 μM 24 h To evaluate the antitumor effect of Vemurafenib on K-1 cells, results showed that E3330 could enhance the antitumor effect of vemurafenib. Cell Death Dis. 2022 Feb 8;13(2):124.
BCPAP 10 μM 24 h To evaluate the antitumor effect of Vemurafenib on BCPAP cells, results showed that E3330 could enhance the antitumor effect of vemurafenib. Cell Death Dis. 2022 Feb 8;13(2):124.
HT29 cells 10 µM 12 h To evaluate the inhibitory effect of Vemurafenib on TSZ-induced necroptotic cell death, results showed that Vemurafenib significantly inhibited necroptotic cell death. Cell Death Dis. 2023 Aug 24;14(8):555.
MDF cells 10 µM 6 h To evaluate the inhibitory effect of Vemurafenib on TSZ-induced necroptotic cell death, results showed that Vemurafenib significantly inhibited necroptotic cell death. Cell Death Dis. 2023 Aug 24;14(8):555.
L929 cells 10 µM 24 h To evaluate the inhibitory effect of Vemurafenib on TNFα-induced necroptotic cell death, results showed that Vemurafenib significantly inhibited necroptotic cell death. Cell Death Dis. 2023 Aug 24;14(8):555.

Vemurafenib/维罗非尼 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice Xenogeneic subcutaneous tumor model Oral 20 mg/kg Once daily for 21 days To evaluate the inhibitory effect of combined treatment with Vemurafenib and E3330 on xenogeneic subcutaneous tumors, results showed that the combined treatment significantly inhibited tumor growth and progression. Cell Death Dis. 2022 Feb 8;13(2):124.
C57BL/6 mice LPS/z-VAD-induced macrophage necroptosis model Intraperitoneal injection 5 mg/kg 15 mins pretreatment To evaluate the inhibitory effect of Vemurafenib on LPS/z-VAD-induced macrophage necroptosis, results showed that Vemurafenib significantly inhibited macrophage necroptosis and reduced the secretion of proinflammatory cytokines. Cell Death Dis. 2023 Aug 24;14(8):555.
Mice Melanoma model Intraperitoneal injection 1 mg/kg Daily for one week PLX4032 inhibits melanoma metastasis by suppressing integrin signaling through PGC1α and ID2 Nature. 2016 Sep 15;537(7620):422-426

Vemurafenib/维罗非尼 动物研究

Dose Mice: 7.5 mg/kg - 60 mg/kg[4] (p.o.) Rat: 10 mg/kg - 450 mg/kg[5] (p.o.) Dog: 150 mg/kg - 300 mg/kg[5] (p.o.)
Administration p.o.
Pharmacokinetics
Animal Rats[5] Dogs[5]
Dose 50 mg/kg (male, day 91) 150 mg/kg (male, day 29)
Administration p.o. p.o.
Cmax 29.2 μM 28100 ng/ml
Tmax 1 h 9 h
AUC0→24h 110.2 μM·h 414000 ng·h/ml

Vemurafenib/维罗非尼 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02052193 Metastatic Melanoma (Carrying ... 展开 >>BRAF V600 Mutation) 收起 << Phase 2 Terminated(Second cohort not o... 展开 >>pened because Simon-Two_Step model failed) 收起 << December 2017 Germany ... 展开 >> Department of Dermatology Tuebingen, BW, Germany, 72076 收起 <<
NCT01603212 Melanoma Phase 1 Phase 2 Completed - United States, Texas ... 展开 >> University of Texas MD Anderson Cancer Center Houston, Texas, United States, 77030 收起 <<
NCT03139513 - Active, not recruiting December 31, 2018 France ... 展开 >> Centre Hospitalier d'Albi Albi Cedex 9, France, 81013 Hopital Prive D Antony; Dermatologie Antony, France, 92166 Chic Cote Basque Bayonne; Medecine II Bayonne, France, 64109 CHU Besançon - Hôpital Jean Minjoz Besançon Cedex, France, 25030 Hopital Avicenne; Dermatologie Bobigny, France, 93009 CH Fleyriat Bourg en Bresse, France, 01000 CH Metropole de Savoie CHAMBERY Cedex, France, 73011 Chu Estaing; Dermatologie Clermont Ferrand, France, 63003 Hopital Louis Pasteur; Sce Dermatologie Colmar, France, 68024 Centre Georges Francois Leclerc Dijon, France, 21000 Chu Site Du Bocage;Dermatologie Dijon, France, 21079 Centre Hospitalier Le Mans; Dermatologie Le Mans, France, 72037 Hopital Claude Huriez; Sce Dermatologie Lille, France, 59037 CHU de Limoges - Hôpital Dupuytren Limoges, France, 87042 Hopital Timone Adultes; Dermatologie Marseille, France, 13385 Hopital Jacques Monod; Dermatologie Montivilliers, France, 76290 Hopital Saint Eloi; CHU de Montpellier; Svc de Dermatologie Montpellier, France, 34295 CH de Mulhouse Hôpital Emile Muller Mulhouse, France, 68070 Hopital l Archet 2; Ginestriere, Service de; Dermatologie Nice cedex 3, France, 06200 Hopital Cochin; Dermatologie Paris, France, 75006 Groupe Hospitalier Bichat Claude Bernard Paris, France, 75018 CENTRE HOSPITALIER ANNECY-GENEVOIS; Dematologie Pringy, France Centre Eugene Marquis Centre Regional de Lutte Contre Le Cancer Rennes, France, 35000 CHU Rouen - CH C. Nicolle - Clinique dermatologique Rouen, France, 76031 CHU de Saint-Etienne - Hopital Nord Saint Etienne, France, 42055 CHI de Poissy St Germain Saint Germain, France, 07810 Hopital Broussais St Malo Cedex, France, 35403 Pole de Cancerologie Prive Strasbourgeois Strasbourg, France, 67000 Hopital Bel Air Thionville Cedex, France, 57126 Hia Sainte Anne; Medecine Interne Oncologie Toulon, France, 83041 CHU de Toulouse - Hôpital Larrey Toulouse, France, 31059 Centre Hospitalier Valence Valence, France, 26953 Institut Gustave Roussy; Dermatologie Villejuif, France, 94805 收起 <<

Vemurafenib/维罗非尼 参考文献

[1]Bollag G, Hirth P, et al. Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma. Nature. 2010 Sep 30;467(7315):596-9.

[2]Yang H, Higgins B, et al. RG7204 (PLX4032), a selective BRAFV600E inhibitor, displays potent antitumor activity in preclinical melanoma models. Cancer Res. 2010 Jul 1;70(13):5518-27.

[3]Yang H, Higgins B, et al. Antitumor activity of BRAF inhibitor vemurafenib in preclinical models of BRAF-mutant colorectal cancer. Cancer Res. 2012;72(3):779-89.

[4]Tate SC, Burke TF, et al. Optimising the combination dosing strategy of abemaciclib and vemurafenib in BRAF-mutated melanoma xenograft tumours. Br J Cancer. 2016 Mar 15;114(6):669-79.

[5]Vemurafenib

Vemurafenib/维罗非尼 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.04mL

0.41mL

0.20mL

10.21mL

2.04mL

1.02mL

20.41mL

4.08mL

2.04mL

Vemurafenib/维罗非尼 技术信息

CAS号918504-65-1
分子式C23H18ClF2N3O3S
分子量 489.92
SMILES Code CCCS(=O)(NC1=CC=C(F)C(C(C2=CNC3=NC=C(C4=CC=C(Cl)C=C4)C=C32)=O)=C1F)=O
MDL No. MFCD18074504
别名 PLX4032; RG7204; RO5185426
运输蓝冰
InChI Key GPXBXXGIAQBQNI-UHFFFAOYSA-N
Pubchem ID 42611257
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, 2-8°C
溶解方案

DMSO: 50 mg/mL(102.06 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
方案 二
配制的工作液建议现用现配，短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在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

Tags: Vemurafenib | PLX4032;RG7204;RO 5185426 RO5185426 Vemurafenib;RO5185426 | Raf | AmBeed-信号通路专用抑制剂 | Vemurafenib/维罗非尼 纯度/质量文件 | Vemurafenib/维罗非尼 亚型比较 | Vemurafenib/维罗非尼 生物活性 | Vemurafenib/维罗非尼 动物研究 | Vemurafenib/维罗非尼 临床数据 | Vemurafenib/维罗非尼 参考文献 | Vemurafenib/维罗非尼 实验方案 | Vemurafenib/维罗非尼 技术信息

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