(R)-BI-2852

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

(R)-BI-2852 是 BI-2852 (HY-126247) 的非活性异构体，可作为实验中的对照化合物。BI-2852 是基于活性分子结构设计的 switch SI/II 口袋的 KRAS 抑制剂，其通过基于结构的活性分子设计具有纳摩尔亲和力。BI-2852 在机理上不同于共价 KRASG12C 抑制剂 (结合 switch II)，与活性 KRASG12D 结合强度是与 KRAS wt 的 10 倍 (740 nM vs 7.5 μM)。BI-2852 阻断 GEF，GAP 和效应子与 KRAS 的相互作用，导致下游信号传导的抑制和 KRAS 突变细胞中的抗增殖作用。

(R)-BI-2852 is the inactive isomer of BI-2852 (HY-126247), and can be used as an experimental control. 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.

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MAPK/ERK Signaling

Ras

Ras

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2375482-49-6

516.59

C31H28N6O2

>98% (HPLC)

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C(NCC=1C=C2N(CC3=CN(C)C=N3)C=CC2=CC1)C4=C(C=5C(N4)=CC=CC5)[C@H]6C=7C(C(=O)N6)=CC=C(O)C7

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(-20℃)

With Ice Pack

≥ 2 years