Fig. 2

The representative structures of mIDH1/2 inhibitors. The phenyl glycine based AG-120 is an orally available mIDH1 inhibitor (IC₅₀ [IDH1^R132H] = 12 nM). The triazines based AG-221 is an orally available mIDH2 inhibitor (IC₅₀ [IDH2^R140Q] = 100 nM versus IC₅₀ [IDH2^wild-type] = 1.8 μM). AG-881 is a pan-IDH inhibitor against both mIDH1 and mIDH2 (IC₅₀ [IDH1^R132H] = 6 nM versus IC₅₀ [IDH2^R140Q] = 12 nM)