1093100-40-3

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 )

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