AGI-6780

AGI-6780 is a potent, selective inhibitor of mutant Isocitrate dehydrogenase 2 (IDH2) (IC₅₀ = 23 nM). It binds allosterically at the dimer interface of mutant IDH2-R140Q, inhibiting 2-hydroxyglutarate (2-HG) formation in human glioblastoma U87 and TF-1 cells expressing IDH2-R140Q with IC₅₀ values of 11 and 18 nM, respectively.