B-Raf inhibitor 1
CAS No. | 1093100-40-3 | Cat. No. | BCP09276 |
Name | B-Raf inhibitor 1 | ||
Synonyms | B-Raf inhibitor1; B-Raf inhibitor-1; | ||
Formula | C26H19ClN8 | M. Wt | 478.94 |
Description | 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. | ||
Pathways | MAPK Pathway | ||
Targets | Raf |
Structure
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