Vemurafenib (PLX4032, RG7204)
BRAF激酶抑制剂
| 规格 | 价格 | 货期 | 数量 |
|---|---|---|---|
| 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 |
特色产品
- 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
- 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
- 对细胞无毒性
- 步骤更简单，无需有机溶剂
- 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
- 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
- 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
- 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
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
APExBIO 顾客使用本产品发表的 13 篇科研文献
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
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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
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
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
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