kras g12d inhibitor 6

KRAS G12D inhibitor 6 is an efficacious compound that effectively inhibits KRAS G12D.

Pan-KRAS-IN-2 (compound 6) is a broad-spectrum KRAS inhibitor exhibiting potent activity with IC50 values of ≤10 nM against KRAS wild type and its mutants (G12D, G12C, G12V, G12S, G12A, Q61H), while showing significantly reduced inhibition, with an IC50 ＞10 μM, for the KRAS G13D mutant [1].

Pan-RAS-IN-6 (compound 24) serves as a DUSP6 inhibitor, effectively reducing MAPK activation in the NCI-H1373-Luc model (DUSP6). It concurrently exhibits notable tumor growth inhibition and regression in the NSCLC brain metastasis mouse model. The compound displays high selectivity and potent inhibitory effects, particularly on KRAS mutation-associated signaling pathways. It demonstrates varied inhibitory activities against distinct KRAS mutants and their interacting proteins. The IC 50 values for KRAS G12C, G12D, and G12V are 1.3 nM, 4.7 nM, and 0.3 nM, respectively.