BI-2852 (C09-1507-941)

Information:BI-2852 BI-2852 is a potent inhibitor of KRAS that binds with nanomolar affinity to a pocket between switch I and II on RAS. BI-2852 blocks all GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in the low micromolar range in KRAS mutant cells.Targets:GTP-KRAS:G12D: (Cell-free assay): GTP-KRAS:G12D: (Cell-free assay) 450 nM: 750 nM(Kd):In vitro:BI-2852 is a KRAS inhibitor that binds with nanomolar affinity to a pocket, thus far perceived to be “undruggable,” between switch I and II on RAS. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitors because it binds to a different pocket present in both the active and inactive forms of KRAS. In doing so, it blocks all GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in the low micromolar range in KRAS mutant cells.Cell Research(from reference):Cell lines：NCI-H358 cells :Concentrations：3 μM, 10 μM, 30 μM, 50 μM :Incubation Time：0-24 hrs Specifications and Purity: 98% Molecular Formula: C31H28N6O2 Molecular Weight: 516.59 PubChem CID: 138756246 Isomeric SMILES: CN1C=C(N=C1)CN2C=CC3=C2C=C(C=C3)CNCC4=C(C5=CC=CC=C5N4)[C@@H]6C7=C(C=CC(=C7)O)C(=O)N6