RAF709 , 98% , 1628838-42-5
| Pack Size | Price | Stock | Quantity |
| 1mg | RMB279.20 | In Stock |
|
| 5mg | RMB767.20 | In Stock |
|
| 25mg | RMB2879.20 | In Stock |
|
| 50mg | RMB4399.20 | In Stock |
|
| 100mg | RMB5919.20 | In Stock |
|
| others | Enquire |
PRODUCT 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 |
Description and Uses
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.
Safety
| Symbol(GHS) |  GHS07 |
| Signal word | Warning |
| Hazard statements | H319-H335-H302+H312+H332-H315 |
| Precautionary statements | P301+P312-P302+P352-P305+P351+P338 |
| HS Code | 2934999090 |
