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B-Raf inhibitor 1 is a potent and selective B-Raf inhibitor with cell IC50s of 0.31 µM and 2 nM for A375 proliferation and A375 p-ERK, respectively. B-Raf inhibitor 1 inhibits A375 and HCT-116 proliferation with IC50s of 0.31 and 0.72 μM, respectively. B-Raf inhibitor 1 additionally exhibits 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.
| Molecular Weight | 478.94 |
| Formula | C26H19ClN8 |
| CAS Number | 1093100-40-3 |
| Solubility (25°C) | DMSO ≥ 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Shanique Alabi, et al. Mutant-selective degradation by BRAF-targeting PROTACs
[2] Arunkumar Babu, et al. A Fluoro Derivative of Embelin, as Potent B-RAF Inhibitor in Melanoma
[3] Eunyoung Park, et al. Architecture of autoinhibited and active BRAF-MEK1-14-3-3 complexes
[4] E M L Heath, et al. B-RAF: A contributor to the melanoma phenotype
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