IDH305 (IDH-305) is a potent, selective, brain penetrant mutant IDH1 inhibitor with IC50 of 18 and 28 nM for IDH1 R132H and R132C.
IDH305 exhibits >200 fold selectivity over WT IDH1 (IC50=6.14 uM), and no activtiy against IDH2 mutants.
IDH305 inhibits EGF-independent proliferation of HCT116-IDH1R132H+/- cells with IC50 of 20 nM.
IDH305 exhibits in vivo correlation of 2-HG reduction and efficacy in IDH1 mutant xenograft tumor model.
