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MRTX0902 is an oral brain penetrating SOS1:KRAS protein-protein interaction inhibitor with an IC50 of 46 nM. MRTX0902 displays high selectivity on SOS1 (Ki=2 nM) over SOS2 and EGFR (both Ki values >10,000 nM), MRTX0902 inhibits MKN1 cells with an IC50 value of 29 nM. MRTX0902 (25, 50 mg/kg; p.o.; twice daily; 25 d) shows anti-tumor effect in mouse model and results tumor regression.
| Molecular Weight | 388.47 |
| Formula | C22H24N6O |
| CAS Number | 2654743-22-1 |
| Solubility (25°C) | DMSO 12 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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