idh2 r140q mutant

AGI-6780 is a potent and selective inhibitor of IDH2 R140Q mutant.

Crelosidenib is a potent and selective mutant IDH inhibitor with IC50s of 6.27 nM, 3.71 nM, 36.9 nM, and 11.5 nM for IDH1 R132H, IDH1 R132C, IDH2 R140Q, and IDH2 R172K mutases, respectively, and low inhibitory activity against the wild-type IDH enzyme.

TQ05310 is an orally active inhibitor of mutant IDH2, targeting both IDH2-R140Q (IC50=136.9 nM) and IDH2-R172K (IC50=37.9 nM) mutations. This compound suppresses the production of 2-hydroxyglutarate (2-HG) by inhibiting the enzymatic activity of mutant IDH2, and induces differentiation in cells expressing IDH2-R140Q and IDH2-R172K. TQ05310 is utilized in research on acute myeloid leukemia.