B-Raf inhibitor 1

An inhibitor of Raf kinases

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库存: 现货

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5mg

￥1100.00

880.00

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10mg

￥1850.00

1480.00

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50mg

￥7337.00

5870.00

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100mg

￥12600.00

10080.00

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货号: ajci7440
CAS: 1093100-40-3
别名: N1-(4-氯苯基)-6-甲基-N5-[3-(9H-嘌呤-6-基)-2-吡啶]-1,5-异喹啉二胺
分子式: C26H19ClN8
分子量: 478.94
纯度: >98%
溶解度: ≥ 47.9mg/mL in DMSO
储存: Store at -20°C
库存: 现货

Background

B-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.

B-Raf inhibitor 1 (Compound 13) inhibits A375 and HCT-116 proliferation with IC50s of 0.31 and 0.72 μM, respectively. B-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. B-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[1].

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.