Raf inhibitor 1 dihydrochloride

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Raf inhibitor 1 dihydrochloride 

B-Raf inhibitor 1 dihydrochloride 是一种有效的 Raf 激酶抑制剂,作用于 B-RafWT, B-RafV600E, 和 C-Raf, Ki 分别为 1 nM, 1 nM, 和 0.3 nM。

Raf inhibitor 1 dihydrochloride

Raf inhibitor 1 dihydrochloride Chemical Structure

CAS No. : 1191385-19-9

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Raf inhibitor 1 dihydrochloride 的其他形式现货产品:

Raf inhibitor 1

生物活性

B-Raf inhibitor 1 dihydrochloride 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.

IC50 & Target[1]

B-Raf

1 nM (Ki)

B-RafV600E

1 nM (Ki)

c-Raf

0.3 nM (Ki)

体外研究
(In Vitro)

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

551.86

Formula

C26H21Cl3N8

CAS 号

1191385-19-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

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.

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