B-Raf inhibitor 1

  • Chemical Properties
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
  • Biological Activity
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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