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 Vitro
Raf 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.
