KRASG12D-IN-7

KRASG12D-IN-7 (Compound (R)-5a) (72 h) exhibits potent and selective anti-proliferative activity against KRAS^G12D harboring AsPC-1 cells (IC₅₀ = 10 nM), GP2D cells (IC₅₀ = 2.7 nM), AGS cells (IC₅₀ = 6.1 nM), HPAF-II cells (IC₅₀ = 6.8 nM) and Ls513 cells (IC₅₀ = 27.3 nM), while showing no significant inhibitory effect on other KRAS-mutant (H358 G12C, G12S) and KRAS WT cell lines (IC₅₀ > 1000 nM)^[1].
KRASG12D-IN-7 binds to KRAS^G12D in both GDp. and GTP bound forms, selectively inhibits the interaction between GDp-loaded KRAS^G12D and SOS1 and hinderes the binding of GTp-loaded KRAS^G12D to RAF1^[1].
KRASG12D-IN-7 (1-1000 nM, 3 h) dose-dependently reduces the protein levels of p-ERK and p-S6 in AsPC-1 cells, effectively suppressing the KRAS downstream MAPK signaling pathway^[1].
KRASG12D-IN-7 (1-1000 nM, 24-72 h) induces G0/G1 phase arrest and apoptosis in AsPC-1 cells^[1].
KRASG12D-IN-7 (5 nM, 10 days) strongly inhibits colony formation of AsPC-1 cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.