B-Raf inhibitor 1 dihydrochloride

"目录号: HY-14177A

MAPK/ERK Pathway-

B-Raf inhibitor 1是B-Raf抑制剂，对A375细胞增殖和A375 p-ERK的IC50分别为0.31 uM和2 nM。

Raf

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生物活性

Description

B-Raf inhibitor 1 is a potent and selective B-Raf inhibitor with cell IC50s of 0.31 uM and 2 nM for A375 proliferation and A375 p-ERK respectively.IC50 value: 0.31 uM and 2 nM for A375 proliferation and A375 p-ERK [1]Target: B-RafB-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. Compound 13 exhibit low micromolar inhibition against wild type B-Raf cell lines, which may be due to off-target kinase activities oralternatively to pan-Raf inhibition, including Raf dimers. Compound 13 induced proliferation and hyperplasia in normal tissues of mice [1].

References

[1].Wang X, et al. Conformation-specific effects of Raf kinase inhibitors. J Med Chem. 2012 Sep 13;55(17):7332-41.