AGI-6780 (Synonyms: AGI 6780;AGI6780)

Cell lines

Primary human AML cells

Preparation method

The solubility of this compound in DMSO is > 22.25 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

5 μM up to 10 days

Applications

IDH2 mutant samples treated with AGI-6780 showed a dose-dependent reduction in the amounts of extracellular and intracellular (R)-2-hydroxyglutarate. In the presence AGI-6780, a burst of cell proliferation was also observed only in the IDH2/R140Q mutant samples. Furthermore, AGI-6780 did not exert a cytotoxic effect as the number of viable, more mature CD45-positive cells increased in the presence of AGI-6780 only in the IDH2/R140Q mutant samples whereas the IDH2/WT samples remained unchanged.

References:

[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.