AGI-6780

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

AGI-6780 是 IDH2 R140Q 突变体的有效选择性抑制剂，IC50 为 23 nM。

AGI-6780 is a potent and selective inhibitor of IDH2 R140Q mutant with IC50 of 23 nM.(In Vitro):AGI-6780 is tested in both human glioblastoma U87 and TF-1 cells expressing IDH2R140Q, as well as against IDH1R132H for 48 h incubation, with IC50 of 11±2.6 nM, 18±0.51 nM, and >1 mM, respectivly.Treatment of TF-1R140Q 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 IDH2R140Q-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 TF1R140Q cells and restored their ability to undergo EPO-induced differentiation.

AGI-6780 is tested in both human glioblastoma U87 and TF-1 cells expressing IDH2R140Q, as well as against IDH1R132H for 48 h incubation, with IC50 of 11±2.6 nM, 18±0.51 nM, and >1 mM, respectivly.Treatment of TF-1R140Q 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 IDH2R140Q-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 TF1R140Q cells and restored their ability to undergo EPO-induced differentiation.

——

AGI6780 | AGI 6780 | AGI-6780

Metabolic Enzyme/Protease

Dehydrogenase

IDH2 R140Q mutant

Cancer

——

1432660-47-3

481.51

C21H18F3N3O3S2

>98% (HPLC)

Ethanol: 96 mg/mL (199.37 mM); DMSO: 96 mg/mL (199.37 mM)

O=S(C1=CC=C(C2=CSC=C2)C(NC(NC3=CC=CC(C(F)(F)F)=C3)=O)=C1)(NC4CC4)=O

N-cyclopropyl-4-(thiophen-3-yl)-3-(3-(3-(trifluoromethyl)phenyl)ureido)benzenesulfonamide

(-20℃)

With Ice Pack

≥ 2 years