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AGI-6780

CAS No. : 1432660-47-3

MCE 站：AGI-6780

产品活性：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。

研究领域：Metabolic Enzyme/Protease

作用靶点：Isocitrate Dehydrogenase (IDH)

In Vitro: AGI-6780 is tested in both human glioblastoma U87 and TF-1 cells expressing IDH2^R140Q, as well as against IDH1^R132H for 48 h incubation, with IC50 of 11±2.6 nM, 18±0.51 nM, and >1 mM, respectivly.Treatment of TF-1^R140Q 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^R140Q-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^R140Q cells and restored their ability to undergo EPO-induced differentiation.

相关产品：Covalent Screening Library Plus  |  Bioactive Compound Library Plus  |  Metabolism/Protease Compound Library  |  Anti-Cancer Compound Library  |  Covalent Screening Library  |  Glutamine Metabolism Compound Library  |  GSK864  |  Mutant IDH1-IN-1  |  Mutant IDH1-IN-2  |  IDH1 Inhibitor 1  |  Mutant IDH1-IN-4

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