kras(g12c) inhibitor 6

K-Ras(G12C) inhibitor 6 is an irreversible, allosteric inhibitor of the K-Ras(G12C) mutant, achieving 100% protein modification at 10 μM after 24 hours in vitro.

KRAS inhibitor-6 is a potent inhibitor of the KRAS G12C variant.

KRAS inhibitor-12 (compound 6-1) is a potent inhibitor of KRAS G12C (IC50: 0.537 μM), exhibiting p-ERK inhibition in MIA PaCA-2 and A549 cells with IC50 values of 1.3 and 3.7 μM, respectively. KRAS inhibitor-12 has potential for study in pancreatic, colorectal, and lung cancers.

KRAS inhibitor-13 (compound 5-6) is a potent inhibitor of KRAS G12C (IC50: 0.883 μM) and demonstrates a p-ERK inhibitory effect in MIA PaCA-2 and A549 cells with IC50 values of 5.9 μM and >100 μM respectively. KRAS inhibitor-13 has potential applications in pancreatic, colorectal, and lung cancer studies.

KRAS G12C inhibitor 56, a powerful inhibitor of SOS1 with an inhibitory concentration (IC50) of 1.6 nM, holds promise for use in cancer research.

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.