| Description | BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) with nanomolar affinity. BI-2852 is leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells. |
| In vitro | BI-2852在低血清和软琼脂条件下对NCI-H358细胞以剂量依赖的方式显示其抗增殖效果，其EC50分别为6.7 μM和5.8 μM。 |
| Target activity | KRas (G12C):450 nM, KRas (G12C):750 nM (kd) |
| molecular weight | 516.59 |
| Molecular formula | C31H28N6O2 |
| CAS | 2375482-51-0 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 55 mg/mL (106.47 mM), Sonication is recommended. |
| References | 1. Kessler D, et al. Drugging an undruggable pocket on KRAS. Proc Natl Acad Sci U S A. 2019 Aug 6; 116(32):15823-15829. |