BI-2852 [CAS 2375482-51-0]

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.

[2375482-51-0]

C31H28N6O2

516.59

OC(C=C1)=CC([C@@H](C2=C(CNCC3=CC4=C(C=CN4CC5=CN(C)C=N5)C=C3)NC6=CC=CC=C62)N7)=C1C7=O

Ras

K-Ras

99.46

DMSO : 55 mg/mL (ultrasonic)

4°C (Powder, stored under nitrogen)

Room Temperature

H302, H315, H319, H335

H302, H315, H319, H335