Background:

AGI-6780 is a potent and selective inhibitor of tumor-associated IDH2/R140Q mutation with IC50 value of 23 nM [1].

AGI-6780 could significantly reduce intracellular concentration of 2HG in the human glioblastoma TF1/R140Q cells, as well as reverse IDH2/R140Q-mediated differentiation block in TF1 cells in the presence of EPO. AGI-6780 could restore KLF1 and hemoglobin G1/2 expressions in the EPO-induced TF1/R140Q cells [1].

参考文献:
[1] Wang F1,?Travins J,?DeLaBarre B,?Penard-Lacronique V,?Schalm S,?Hansen E,?Straley K,?Kernytsky A,?Liu W,?Gliser C,?Yang H,?Gross S,?Artin E,?Saada V,Mylonas E,?Quivoron C,?Popovici-Muller J,?Saunders JO,?Salituro FG,?Yan S,?Murray S,?Wei W,?Gao Y,?Dang L,?Dorsch M,?Agresta S,?Schenkein DP,?Biller SA,?Su SM,?de Botton S,?Yen KE. Targeted?inhibition?of?mutant?IDH2?in?leukemia?cells?induces?cellular?differentiation. Science.?2013 May 3;340(6132):622-6.