B-Raf inhibitor 1 curtails proliferation in A375 and HCT-116 cells with IC50s of 0.31 μM and 0.72 μM, respectively. This inhibitor also connects to and maintains B-Raf in a DFG-out inactive configuration where the ATP pocket is partially occupied by Phe595 and Gly596 of the DFG motif. Moreover, B-Raf inhibitor 1 demonstrates inhibition at low micromolar concentrations in wild type B-Raf cell lines, possibly from unintended kinase effects or widespread Raf inhibition, including interactions between Raf dimers[1].
体外研究
B-Raf inhibitor 1 curtails proliferation in A375 and HCT-116 cells with IC50s of 0.31 μM and 0.72 μM, respectively. This inhibitor also connects to and maintains B-Raf in a DFG-out inactive configuration where the ATP pocket is partially occupied by Phe595 and Gly596 of the DFG motif. Moreover, B-Raf inhibitor 1 demonstrates inhibition at low micromolar concentrations in wild type B-Raf cell lines, possibly from unintended kinase effects or widespread Raf inhibition, including interactions between Raf dimers[1].
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