Molecular Formula | C24H16F6N6O
|
Molar Mass | 518.41 |
Density | 1.50 |
Boling Point | 667.6±65.0 °C(Predicted) |
pKa | 9.07±0.27(Predicted) |
Storage Condition | -20℃ |
Sensitive | Light Sensitive |
Use | RAF265 (CHIR-265) is a highly selective B- Raf and VEGFR2 inhibitor with IC50 of 3-60 nM, which also inhibits VEGFR2 phosphorylation, EC50 of 30 nM,Phase 2. |
In vitro study | RAF265 is a potent novel BRAF/VEGFR-2 inhibitor that acts on A375M(RAF265 has significant activity against BRAF in HT29 and MDAMB231 cells, with an IC20 of 1 to 3 μm, the IC50 is 5 to 10 μm. Treatment of BRAF mutant cell lines with concentrations of 1 to 10 μm RAF265 reduced MEK phosphorylation. Treatment of non-BRAF mutant cell lines with 1 μm RAF265 increased MEK phosphorylation, which was reversed when RAF265 concentrations reached 5 μm. The toxicity of RAF265 on HCT116 cell line was enhanced by the addition of RAD001. Treatment with RAF265 reduced pERK levels in a dose-dependent manner, and treatment with 0.5 mM RAF265 for 2 hours completely blocked phase G2-M progression, resulting in G2-M cells. Inhibition of expression of RAF265 |
In vivo study | RAF265 inhibited the accumulation of FDG in A375M tumor. RAF265 is a novel, oral, small-molecule BRAF kinase and VEGFR-2 inhibitor that acts on mutant BRAF tumor models with potent anticancer activity. In the study of human xenografts, RAF265 is highly effective in mutant BRAF human xenografts and some wild-type BRAF models. |