KRASG12D-IN-7 

KRASG12D-IN-7 is a selective KRAS^G12D inhibitor. KRASG12D-IN-7 displays strong binding activity for KRAS^G12D in both its GDP- and GTP- bound states, with K_d value of 1.12 nM and 1.86 nM, respectively. KRASG12D-IN-7 inhibits the proliferation of KRAS^G12D harboring AsPC-1 cells with an IC₅₀ value of 10 nM and suppresses MAPK signaling. KRASG12D-IN-7 induces G0/G1 phase arrest and apoptosis in AsPC-1 cells, and strongly inhibits their colony formation. KRASG12D-IN-7 can be used for the study of cancers harboring KRAS^G12D mutation, particularly pancreatic ductal adenocarcinoma (PDAC)^[1].

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.

671.04

C₃₁H₃₂ClF₂N₇OSe

N#CC1=C(N)[Se]C2=CC=CC(C3=C(F)C4N=C(OC[C@@]56CCCN5C[C@H](F)C6)N=C(N7C[C@H]8N[C@H](CC8)C7)C4C=C3Cl)=C21

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• [1]. Zhou L, et al. The design and synthesis of selective and potent selenium-containing KRASG12D inhibitors. Eur J Med Chem. 2025 Nov 15;298:118004.  [Content Brief]