kras inhibitor-8

KRAS inhibitor-8 is a potent inhibitor of the mutated KRAS G12C protein.

SOS1-IN-18 (Compound 8) is an inhibitor of the Son of Sevenless 1 protein (SOS1) with a dissociation constant (KD) of 2.6 nM. It disrupts the SOS1-KRAS G12C interaction with an IC50 of 3.4 nM, inhibits ERK phosphorylation in H358 cells with an IC50 of 31 nM, and curtails the proliferation of H358 cells with an IC50 of 5 nM.

KRAS inhibitor-42 (compound 8) is an effective USP7 inhibitor that exhibits high affinity for GDP-bound KRASG12D, with a Ki value of 2.7 μM.

pan-KRAS-IN-8 (Compound 38) is an inhibitor of the human tumor mutated gene KRAS. It effectively suppresses the proliferation of KRAS mutant cells AsPC-1 (G12D mutant) and SW480 (G12V mutant), with IC50 values of 0.07 nM and 0.18 nM, respectively.

Pan-KRAS-IN-8 (Compound 52) is an inhibitor of the human tumor mutant gene KRAS. It suppresses the proliferation of KRAS mutant cells AsPC-1 (G12D mutant) and SW480 (G12V mutant) with IC50 values of 0.24 nM and 0.30 nM, respectively.

Setidegrasib (example 8), a quinazoline-linked (4R)-4-hydroxy-L-prolinamide compound, acts as a proteolysis targeting chimera (PROTAC) [1], specifically inducing degradation of the G12D-mutation KRAS protein.

GNE-9815 (3-(2-cyanopropan-2-yl)-N-[2-fluoro-4-methyl-5-(7-methyl-8-oxo-7,8-dihydropyrido[2,3-d]pyridazin-3-yl)phenyl]benzamide) is a high kinase-selective inhibitor of RAF and targets KRAS-mutant cancers through combination therapy.