Description
RAS inhibitor Abd-7 is a potent RAS-binding compound (Kd=51nM) that interacts with RAS in cells, prevents RAS-effector interactions and inhibits endogenous RAS-dependent signalling; impairs the protein-protein interaction (PPI) of various mutant KRAS proteins with PI3K, CRAF and RALGDS as well as NRASQ61H and HRASG12V, inhibits phosphorylation of both downstream biomarkers in colorectal cancer (DLD-1, KRASG13D) and NSCLC (H538, KRASG12C) human cell lines, with reduction of AKT phosphorylation starting at 2uM; shows consistent inhibitory effects in the cell-based BRET assay and the biomarker assay