TQ05310 is an orally available inhibitor of IDH2 mutants, targeting both IDH2-R140Q (IC50=136.9 nM) and IDH2-R172K (IC50=37.9 nM) mutants. TQ05310 inhibits the production of 2-hydroxyglutarate (2-HG) and induces differentiation of cells expressing IDH2-R140Q and IDH2-R172K by inhibiting the enzymatic activity of mutant IDH2. TQ05310 can be used for the study of acute myeloid leukemia[1].
[1] Mingzhao Gao, et al. "Pharmacological characterization of TQ 05310, a potent inhibitor of isocitrate dehydrogenase 2 R140Q and R172K mutants." Cancer science 110.10 (2019): 3306-3314. DOI:10.1111/cas.14152
