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BI-2852 is a KRAS inhibitor for the switch I/II pocket. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitors because it binds to a different pocket present in both the active and inactive forms of KRAS. BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells. BI-2852 (10 nM-10 µM; 2 hours) shows a dose-dependent pERK modulation and antiproliferative effect at EC50s of 5.8 µM and 6.7 µM in soft agar and low serum conditions in NCI-H358 cells.
| Molecular Weight | 516.59 |
| Formula | C31H28N6O2 |
| CAS Number | 2375482-51-0 |
| Solubility (25°C) | DMSO ≥ 37 mg/mL |
| Storage | 2-8°C, dry, sealed |
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