Mutant IDH1-IN-7 

Mutant IDH1-IN-7 is a highly selective Isocitrate Dehydrogenase 1 (IDH1) R132H (IC₅₀ = 0.26 μM, K_d = 2.1 μM)/R132C (IC₅₀ = 1.1 μM) inhibitor. Mutant IDH1-IN-7 has no inhibitory effect on wild-type IDH1, IDH2-wt, and IDH2 R140Q. Mutant IDH1-IN-7 inhibits 2-Hydroxyglutarate (2-HG) production in U87-MG R132H cells (EC₅₀ = 0.55 μM). Mutant IDH1-IN-7 exhibits moderate antiproliferative effects on U87-MG R132H and HT-1080 cells^[1].

Mutant IDH1-IN-7 (Compound 13e) (10-40 μM, 72 h) exhibits moderate antiproliferative activity against U87-MG IDH1 R132H and HT-1080 cells while displaying significantly lower potency in U87-MG and L02 cells^[1].
Mutant IDH1-IN-7 (5 μM, 1 h) shows no inhibitory effect on wild-type IDH1, IDH2-wt and IDH2 R140Q, with IC₅₀ values > 40 μM^[1].

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

456.54

C₂₇H₂₈N₄O₃

CC1=CC=C(C=C1)NC(CN2C(N/C(C2=O)=C\C3=CC=CN3C4=CC(CC(C)C)=CC=C4)=O)=O

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• [1]. Luo D, et al. Discovery and structure-activity relationship study of novel hydantoin-based inhibitors targeting mutant isocitrate dehydrogenase 1 (mIDH1). Eur J Med Chem. 2025 Jul 5;297:117945.