Molecular Formula | C31H28N6O2 |
Molar Mass | 516.59 |
Density | 1.41±0.1 g/cm3(Predicted) |
Boling Point | 906.5±65.0 °C(Predicted) |
pKa | 8.95±0.40(Predicted) |
Storage Condition | 2-8°C,惰性气体保存 |
In vitro study | BI-2852 (Compound 1) (10 nM-10 µM; 2 hours) shows a dose-dependent pERK modulation and antiproliferative effect at EC 50 s of 5.8 µM and 6.7 µM in soft agar and low serum conditions in NCI-H358 cells. |
biological activity | BI-2852 is a switch SI/II pocket KRAS inhibitor designed based on drug structure, it has nanomolar affinity through structure-based drug design. BI-2852 is mechanistically different from covalent KRAS G12C inhibitors (binding to switch II), binding to active KRAS g12d is 10-fold stronger than KRAS wt (740 nM vs 7.5 μm). BI-2852 blocking the interaction of GEF,GAP, and effector with KRAS leads to inhibition of downstream signaling and antiproliferative effects in KRAS mutant cells. |