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| Product Name: | RAF709 | | Synonyms: | RAF709;CS-2505;RAF-709;RAF 709;Benzamide, N-[2-methyl-5'-(4-morpholinyl)-6'-[(tetrahydro-2H-pyran-4-yl)oxy][3,3'-bipyridin]-5-yl]-3-(trifluoromethyl)-;N-[2-Methyl-5'-(4-morpholinyl)-6'-[(tetrahydro-2H-pyran-4-yl)oxy][3,3'-bipyridin]-5-yl]-3-(trifluoromethyl)benzamide;Inhibitor,inhibit,Raf,Raf kinases,RAF709,RAF-709,RAF 709 | | CAS: | 1628838-42-5 | | MF: | C28H29F3N4O4 | | MW: | 542.55 | | EINECS: | | | Product Categories: | | | Mol File: | 1628838-42-5.mol |  |
| | RAF709 Chemical Properties |
| Boiling point | 622.7±55.0 °C(Predicted) | | density | 1.321±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO:100.0(Max Conc. mg/mL);184.31(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:2):0.33(Max Conc. mg/mL);0.61(Max Conc. mM)
DMF:30.0(Max Conc. mg/mL);55.29(Max Conc. mM)
Ethanol:100.0(Max Conc. mg/mL);184.31(Max Conc. mM) | | form | A crystalline solid | | pka | 11.87±0.70(Predicted) |
| | RAF709 Usage And Synthesis |
| Description | RAF709 is a potent inhibitor of B-RAF and C-RAF (IC50s = 0.4 and 0.5 nM, respectively). It is selective for RAF kinases exhibiting >99% inhibition of only B-RAF, B-RAFV600E, and C-RAF in a panel of 456 kinases. However, DDR1, DDR2, FRK, and PDGFRβ are also inhibited by >80% at a concentration of 1 μM. RAF709 inhibits phosphorylation of MEK and ERK (EC50s = 0.02 and 0.1 μM, respectively) with minimal paradoxical activation, stabilizes BRAF-CRAF dimers (EC50 = 0.8 μM), and reduces proliferation of Calu-6 RAS mutant cells (EC50 = 0.95 μM). In a Calu-6 mouse non-small cell lung cancer (NSCLC) xenograft model, RAF709 (10-200 mg/kg) reduces ERK phosphorylation and decreases tumor volume in a dose-dependent manner without affecting total body weight. |
| | RAF709 Preparation Products And Raw materials |
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