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Submit ReviewVemurafenib is a potent inhibitor of BRAFV600E, C-Raf and wild type B-Raf (IC50 values are 13-31 nM, 6.7-48 nM and 100-160 nM, respectively. Vemurafenib also inhibits SRMS, ACK1 KHS1, FGR (IC50 values are 18 nM, 19 nM, 51 nM and 63 nM, respectively). Vemurafenib shows antitumor activity and induces autophagy in BRAF-mutant thyroid cancer cells.
Vemurafenib is also offered as part of the Tocriscreen Kinase Inhibitor Library. 了解 Tocris 化合物库的更多信息。
分子量 | 489.92 |
公式 | C23H18ClF2N3O3S |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 918504-65-1 |
PubChem ID | 42611257 |
InChI Key | GPXBXXGIAQBQNI-UHFFFAOYSA-N |
Smiles | O=C(C1=CNC2=NC=C(C=C21)C=3C=CC(Cl)=CC3)C=4C(F)=CC=C(NS(=O)(=O)CCC)C4F |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 48.99 | 100 |
以下数据基于产品分子量 489.92。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.04 mL | 10.21 mL | 20.41 mL |
5 mM | 0.41 mL | 2.04 mL | 4.08 mL |
10 mM | 0.2 mL | 1.02 mL | 2.04 mL |
50 mM | 0.04 mL | 0.2 mL | 0.41 mL |
参考文献是支持产品生物活性的出版物。
Wang et al (2017) Targeting autophagy sensitizes BRAF-mutant thyroid cancer to vemurafenib. J.Clin.Endocrinol.Metab. 102 634 PMID: 27754804
Ibrahim et al (2013) Chapter twenty-six - case history: vemurafenib, a potent, selective, and first-in-class inhibitor of mutant BRAF for the treatment of metastatic melanoma. Annu.Rep.Med.Chem. 48 435
Davis and Schlessinger (2012) The genesis of zelboraf: targeting mutant B-Raf in melanoma. J.Cell.Biol. 199 15 PMID: 23027900
If you know of a relevant reference for Vemurafenib, please let us know.
关键词: Vemurafenib, Vemurafenib supplier, BRAF, kinases, inhibitors, inhibits, potent, BRAFV600E, CRAF, B-raf, c-raf, autophagy, antitumor, Raf, Kinase, 7309, Tocris Bioscience
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