B-Raf Inhibitor 1

CAS No. : 1093100-40-3

B-Raf Inhibitor 1,1093100-40-3
Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000391
Molecular Formula:C₂₆H₁₉ClN₈
Molecular Weight:478.94
IC50:0.31 uM and 2 nM for A375 proliferation and A375 p-ERK [1]
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Appearance:Solid powder
Purity: > 98%
Cat No:I000391
Cas No:1093100-40-3
Product-Name:B-Raf Inhibitor 1

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-Raf
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. Compound 13 exhibit 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. Compound 13 induced proliferation and hyperplasia in normal tissues of mice [1]

[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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