AGI-6780 有效且选择性抑制肿瘤相关突变体 IDH2^R140Q，IC₅₀ 为 23±1.7 nM。AGI-6780 对 IDH2^WT 的作用效果微弱，IC₅₀ 为 190±8.1 nM。

AGI-6780 that potently and selectively inhibits the tumor-associated mutant IDH2 with IC 50 of 23±1.7 nM. AGI-6780 is less potent against IDH2 with IC 50 of 190±8.1 nM.

Solid

IC50: 23±1.7 nM (IDH2), 190±8.1 nM (IDH2)

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Wang F, et al. Targeted inhibition of mutant IDH2 in leukemia cells induces cellular differentiation. Science. 2013 May 3;340(6132):622-6.

In Vitro: DMSO : ≥ 29 mg/mL (60.23 mM)配制储备液