Description
Raf inhibitor 1 is a potent Raf kinase inhibitor with K i s of 1 nM, 1 nM, and 0.3 nM for B-Raf WT, B-Raf V600E, and C-Raf, respectively.In VitroRaf inhibitor 1 (Compound 13) inhibits A375 and HCT-116 proliferation with IC 50 s 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:B-Raf 1 nM (Ki) B-Raf V600E 1 nM (Ki) c-Raf 0.3 nM (Ki)