产品
编 号:F618410
分子式:C31H28N6O2
分子量:516.59
产品类型
结构图
CAS No: 2375482-51-0
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产品详情
生物活性:
BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based agent design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRASG12D versus KRASwt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.
体外研究:
BI-2852 (化合物 1) (10 nM-10 μM;2 小时) 在 EC50 5.8 μM 和 6.7 μM 软琼脂和低血清中表现出剂量依赖性 pERK 调节和抗增殖作用 NCI-H358 细胞条件。