Catalog No. A3004

Vemurafenib (PLX4032, RG7204)

Name: Vemurafenib (PLX4032, RG7204),维罗非尼,Vemurafenib,918504-65-1
Brand: APExBIO
SKU: A3004
Price: 500 CNY
Availability: InStock

（别名：Vemurafenib, 维罗非尼）

BRAF激酶抑制剂

规格	价格	货期
1mL(10 mM in DMSO)	￥500.00	现货
10mg	￥454.00	现货
50mg	￥1090.00	现货
200mg	￥2727.00	现货
500mg	￥4000.00	现货
1000mg	￥9090.00	现货

CAS号：918504-65-1纯度：98.48%

仅用于科研，不用于诊疗。未经明确授权不得转售。

021-55669583sales@apexbio.cnAPExBIO

特色产品

Annexin V-FITC/PI Apoptosis Kit

用于双染检测细胞凋亡和坏死

- 在10-20分钟内完成染色
- 适用于流式细胞仪和荧光显微镜检测
- 准确区分活细胞/凋亡细胞/坏死细胞

Phos binding reagent (Phosbind) acrylamide

分离和检测磷酸化/非磷酸化蛋白

- 新型的磷酸盐结合标签和功能分子
- 用于免疫印迹和质谱分析等后续操作
- 适用于30 KDa-130 KDa大小的蛋白

Cell Counting Kit-8 (CCK-8)

用于细胞增殖和细胞毒性试验

- 比MTT，MTS或WST-1更敏感
- 对细胞无毒性
- 步骤更简单，无需有机溶剂

Cy5 TSA Fluorescence System Kit

Cy5荧光标记的酪胺信号放大系统

- 检测ICC/IHC/ISH中的低丰度靶点
- 可将信号灵敏度提高100倍
- 同时保持稳定的特异性和分辨率

EZ Cap™ Cy5 Firefly Luciferase mRNA (5-moUTP)

用于观察mRNA运送，定位，翻译

- 具有Cap1结构的荧光素酶mRNA
- 提供更高的转录效率并抑制免疫激活
- 使用5-moUTP和Cy5-utp修饰

HotStart™ 2X Green qPCR Master Mix

用于荧光定量目标DNA或cDNA

- 通过热启动机制优化扩增特异性
- 优异的扩增效率、可重复性和稳定性
- 卓越的灵敏度和准确性，操作简单

HyperScribe™ T7 High Yield Cy5 RNA Labeling Kit Plus

高效的Cy5修饰RNA转录试剂盒

- 适合原位/Northernblot杂交实验
- 优化的缓冲液和T7 RNA聚合酶混合物
- 20 μL反应体系可获得更高的RNA产量

产品描述产品性质产品应用生物相关数据质量控制操作说明产品引用文献摩尔浓度计算器

产品描述

Vemurafenib是BRAF激酶的抑制剂，它可以抑制突变型BRAF V600E的活性，同时也可以抑制CRAF、ARAF和野生型BRAF激酶的活性。Vemurafenib是一个竞争性的小分子抑制剂，针对丝氨酸-苏氨酸激酶，靶向结合突变型BRAF的ATP结合域。在无BRAF突变的细胞中，Vemurafenib可以增强由RAF同源或异源二聚体对下游MEK的激活，这是由于在BRAF-CRAF异源二聚体和CRAF-CRAF同源二聚体中非药物结合伴侣的反式激活引起的。

参考文献：
Keith. T Flaherty, Uma Yasothan and Peter Kirkpatrick. Vemurafenib. Nature Reviews Drug Discovery. 2011; 10: 811 – 812.
Jason J. Luke, F. Stephen Hodi. Vemurafenib and BRAF Inhibition: A New Class of Treatment for Metastatic Melanoma. Clinical Cancer Research. 2012; 18: 9 – 14.

产品性质

物理外观	A solid
CAS号	918504-65-1
分子式	C₂₃H₁₈ClF₂N₃O₃S
分子量	489.93
小分子别名	Vemurafenib
化学名称	N-[3-[5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluorophenyl]propane-1-sulfonamide
溶解度	≥24.5 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
SMILES	CCCS(Nc(c(F)c1C(c(c2c3)c[nH]c2ncc3-c(cc2)ccc2Cl)=O)ccc1F)(=O)=O
存储条件	-20°C
运输条件	蓝冰

产品应用 (实验数据来自文献，APExBIO并未验证，仅供参考)

IC50和靶点

生物活性描述	Vemurafenib (PLX4032, RG7204)是一种新型有效的B-Raf V600E抑制剂，IC50值为31 nM。
靶点	B-RafV600E	C-Raf	MAP4K5 (KHS1)	SRMS	ACK1	FGR
生物活性数据	31 nM	48 nM	51 nM	18 nM	19 nM	63 nM

生物相关数据

质量控制

请选择批次查看:

纯度 = 98.48%

COA (Certificate Of Analysis)HPLC NMR (Nuclear Magnetic Resonance)MSDS (Material Safety Data Sheet)

操作说明

Datasheet 小分子化合物通用使用指南

APExBIO 顾客使用本产品发表的 13 篇科研文献

1. Charlie George Barker, Sumana Sharma, et al. "Integrative multi-omics defines melanoma drug response networks and ARID1A-dependent resistance mechanisms." Mol Syst Biol. 2026 Feb 18. PMID: 41708984

2. Ali Talebi, Vincent de Laat, et al. "Pharmacological induction of membrane lipid poly-unsaturation sensitizes melanoma to ROS inducers and overcomes acquired resistance to targeted therapy." J Exp Clin Cancer Res. 2023 Apr 19;42(1):92. PMID: 37072838

3. MENGTING OU, XICHAO XU, et al. "MDM2 induces EMT via the B‑Raf signaling pathway through 14‑3‑3." Oncol Rep. 2021 Jul;46(1):120. PMID: 33955525

4. Satoh TK, Mellett M, et al. "IL-36γ drives skin toxicity induced by EGFR/MEK inhibition and commensal Cutibacterium acnes." J Clin Invest. 2019 Dec 5. pii: 128678. PMID: 31805013

5. Sechi M, Lall RK, et al. "Fisetin targets YB-1/RSK axis independent of its effect on ERK signaling:insights from in vitro and in vivo melanoma models." Sci Rep. 2018 Oct 24;8(1):15726. PMID: 30356079

6. Zanconato F, Battilana G, et al. "Transcriptional addiction in cancer cells is mediated by YAP/TAZ through BRD4." Nat Med. 2018 Oct;24(10):1599-1610. PMID: 30224758

7. Hwang BJ, Adhikary G, et al. "Chk1 inhibition as a novel therapeutic strategy in melanoma." Oncotarget. 2018 Jul 13;9(54):30450-30464. PMID: 30100999

8. Talebi A, Dehairs J, et al. "Sustained SREBP-1-dependent lipogenesis as a key mediator of resistance to BRAF-targeted therapy." Nat Commun.2018 Jun 27;9(1):2500. PMID: 29950559

9. Zuo Q, Liu J, et al. "AXL/AKT axis mediated-resistance to BRAF inhibitor depends on PTEN status in melanoma." Oncogene. 2018 Mar 19. PMID: 29551771

10. Fisher ML, Grun D, et al. "Inhibition of YAP function overcomes BRAF inhibitor resistance in melanoma cancer stem cells." Oncotarget.2017 Nov 22;8(66):110257-110272. PMID: 29299145

11. Sieber J, Wieder N, et al. "GDC-0879, a BRAF(V600E) Inhibitor, Protects Kidney Podocytes from Death." Cell Chem Biol. 2017 Dec 6. PMID: 29249695

12. Basu R, Baumgaertel N, et al. "Growth Hormone Receptor Knockdown Sensitizes Human Melanoma Cells to Chemotherapy by Attenuating Expression of ABC Drug Efflux Pumps. Horm Cancer." 2017 Jun;8(3):143-156. PMID: 28293855

13. Yuan He, Djoke Hendriks, et al. "Melanoma-directed activation of apoptosis using a novel bispecific antibody directed at MCSP and TRAIL receptor 2/Death Receptor 5." Journal of Investigative Dermatology,February 2016, volume 136, pages 541-4