927880-90-8
RAF265 (CHIR-265)
CAS: 927880-90-8
Molecular Formula: C24H16F6N6O
927880-90-8 - Names and Identifiers
927880-90-8 - Physico-chemical Properties
| 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. |
927880-90-8 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.929 ml | 9.645 ml | 19.289 ml |
| 5 mM | 0.386 ml | 1.929 ml | 3.858 ml |
| 10 mM | 0.193 ml | 0.964 ml | 1.929 ml |
| 5 mM | 0.039 ml | 0.193 ml | 0.386 ml |
Last Update：2024-01-02 23:10:35
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View History
927880-90-8
5-FLUORO-2-METHYLBENZOYL CHLORIDE
六硝基癸啉
Sodium hydride inoil gray powder
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71042-54-1
5-FLUORO-2-METHYLBENZOYL CHLORIDE
六硝基癸啉
Sodium hydride inoil gray powder
n-methylol-chloracetamide
鹤庆五味子辛素
71042-54-1