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维罗非尼 /Vemurafenib {[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 化学结构 CAS号：918504-65-1
Vemurafenib 化学结构
CAS号：918504-65-1
Vemurafenib 3D分子结构
CAS号：918504-65-1
Vemurafenib 化学结构 CAS号：918504-65-1
Vemurafenib 3D分子结构 CAS号：918504-65-1
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Vemurafenib 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:

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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(V600E), IC50: 23 nM

BRAF WT, IC50: 32 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(V600E), IC50: 5.8 nM

BRAF WT, IC50: 15 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

 		99%
PLX7904 ✔ 98+%
Sorafenib ++

B-Raf (V599E), IC50: 38 nM

B-Raf, IC50: 22 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 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 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
8505C (BRAF V600E/V600E) Growth Inhibition Assay 96 h IC50=57 nM 20149136
A375 100 μM Growth Inhibition Assay 96 h IC50=47 nM 18458053
A375 10 μM Apoptosis Assay Promotes apoptotic death 18458053
A375 (BRAFV600E) Function Assay 8 h Increases intracellular ROS and NO levels 25363644

Vemurafenib 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 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 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 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 技术信息

CAS号918504-65-1
分子式C23H18ClF2N3O3S
分子量 489.922
别名 PLX4032;RG7204;Brand name: Zelboraf;RO 5185426 RO5185426 Vemurafenib;RO5185426
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C
溶解度

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
动物实验配方

IP 2% DMSO+2% Tween80+30% PEG300+water 5 mg/mL clear

PO 0.5% CMC-Na 63 mg/mL suspension

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

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