S81948 |
B-Raf inhibitor 1 |
源叶(MedMol) | 97% |
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- 产品描述: Raf inhibitor 1 is a potent Raf kinase inhibitor with Kis of 1 nM, 1 nM, and 0.3 nM for B-RafWT, B-RafV600E, and C-Raf, respectively.
- 靶点: B-Raf:1 nM (Ki);B-RafV600E:1 nM (Ki);c-Raf:0.3 nM (Ki);Raf
- 体外研究:
Raf inhibitor 1 (Compound 13) inhibits A375 and HCT-116 proliferation with IC50s of 0.31 and 0.72 μM, respectively. Raf inhibitor 1 (Compound 13) binds to and stabilizes B-Raf in a DFG-out, inactive conformation in which the ATP pocket is partially filled by Phe595 and Gly596 from the DFG motif. Raf inhibitor 1 (Compound 13) additionally exhibits low micromolar inhibition against wild type B-Raf cell lines, which may be due to off-target kinase activities or alternatively to pan-Raf inhibition, including Raf dimers
- 参考文献:
1. Wang X, et al. Conformation-specific effects of Raf kinase inhibitors. J Med Chem. 2012 Sep 13;55(17):7332-41.
- 溶解性: soluble in DMSO
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.088 ml 10.44 ml 20.88 ml 5 mM 0.418 ml 2.088 ml 4.176 ml 10 mM 0.209 ml 1.044 ml 2.088 ml 50 mM 0.042 ml 0.209 ml 0.418 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)