|
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;N-(2-Methyl-5'-morpholino-6'-((tetrahydro-2H-pyran-4-yl)oxy)-[3,3'-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide | 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) | color | White to off-white |
| 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 |
|