AGI-6780 that potently and selectively inhibits the tumor-associated mutant IDH2 with IC50 of 23±1.7 nM. AGI-6780 is less potent against IDH2 with IC50 of 190±8.1 nM.
IC50&Target
IC50: 23±1.7 nM (IDH2), 190±8.1 nM (IDH2)
体外研究
AGI-6780 is tested in both human glioblastoma U87 and TF-1 cells expressing IDH2, as well as against IDH1 for 48 h incubation, with IC50 of 11±2.6 nM, 18±0.51 nM, and >1 mM, respectivly.Treatment of TF-1 cells with AGI-6780, at concentrations that lower 2HG to near-normal physiologic levels, restore expression of both HBG and KLF1 genes and the color change associated with differentiation. AGI-6780 can reverse the IDH2-induced differentiation block in TF-1 cells. Pretreatment with AGI-6780 (0.2 μM and 1 μM) markedly decreased the intracellular concentration of (R)-2-hydroxyglutarate in the TF1 cells and restored their ability to undergo EPO-induced differentiation.
分子式
C21H18F3N3O3S2
分子量
481.51
CAS号
1432660-47-3
运输条件
Room temperature in continental US; may vary elsewhere.