Raf inhibitor 1 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.
B-Raf inhibitor 1 is a potent Raf kinase inhibitor for B-RafWT, B-RafV600E, and C-Raf with Ki of 1 nM, 1 nM, and 0.3 nM, respectively.
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.
| B-Raf < span> 1 nM (Ki) | B-Raf V600E 1 nM (Ki) | c-Raf 0.3 nM (Ki ) |
B-Raf: 1 nM (Ki); B-RafV600E: 1 nM (Ki); c-Raf: 0.3 nM (Ki)
[1] Wang X, et al. Conformation-specific effects of Raf kinase inhibitors. J Med Chem. 2012 Sep 13;55(17):7332-41. DOI:
10.1021/jm300613w
