2375482-51-0

BI-2852 is a switch SI/II pocket KRAS inhibitor with nanomolar affinity through structure-based drug design. It is mechanistically distinct from covalent KRASG12C inhibitors (binding switch II), binding to active KRASG12D 10-fold more strongly than KRAS wt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP and effector interactions with KRAS, resulting in inhibition of downstream signaling and antiproliferative effects in KRAS mutant cells.

KRAS(G12C) 450 nM (IC 50 )

KRAS(G12C) < p> 750 nM (Kd)