AG-221-恩西地平 Enasidenib_代谢酶/蛋白酶-MedChemExpress LLC

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产品简介 品牌 MedChemExpress (MCE) 货号 HY-18690 规格 10 mM * 1 mL；5 mg；10 mg 供货周期 现货 应用领域 生物产业     Enasidenib是可口服，可逆，选择性的 IDH2 突变酶抑制剂，抑制IDH2R140Q 和 IDH2R172K 的 IC50 分别为100 和 400 nM。
详细介绍 Enasidenib

产品活性：Enasidenib是可口服，可逆，选择性的 IDH2 突变酶抑制剂，抑制IDH2R140Q 和 IDH2R172K 的 IC50 分别为100 和 400 nM。

研究领域：metabolic Enzyme/Protease

作用靶点：Isocitrate Dehydrogenase (IDH)

In Vitro: Enasidenib (AG-221) reverses the effects of mutant IDH2 on DNA methylation in mutant stem/progenitor cells. Enasidenib induces differentiation and impairs self-renewal of IDH2-mutant leukemia cells, effects that are further enhanced by simultaneous inhibition of Flt3ITD. Enasidenib (AG-221) therapy induces differentiation of leukemic cells, with an increase in the CD11b+ population and a decrease in the c-Kit+ population in the peripheral blood at 2wks.

In Vivo: Treatment with Enasidenib (AG-221) significantly improves survival in an IDH2-mutant acute myeloid leukemia (AML) primary xenograft mouse model. Enasidenib (AG-221), a mutant IDH2 inhibitor, remodels the epigenetic state of IDH2-mutant cells and induces alterations in self-renewal/differentiation in IDH2-mutant AML model in vivo. Enasidenib treatment (10mg/kg or 100mg/kg bid) leads to a reduction in 2-HG in vivo (96.7% below pre-treatment levels). Moreover, Enasidenib treatment restores megakaryocyte-erythroid progenitor (MEP) differentiation that is suppressed by mutant IDH2 expression (mean MEP% mean, 39% Veh vs 50% AG-221). Enasidenib therapy reverses the effects of mutant IDH2; a significant reduction is observed in DNA methylation, including 180 genes that have 20 or more hypomethylated differentially methylated cytosines (DMCs) following treatment. Enasidenib (100mg/kg bid) treatment of mice engrafted with Mx1-Cre IDH2R140QFlt3ITD AML cells markedly reduces 2-hydroxyglutarate (2-HG) levels consistent with on target inhibition. Enasidenib inhibits mutant IDH2-mediated 2-HG production.

相关产品：FDA-Approved Drug Library Plus | Drug Repurposing Compound Library | FDA-Approved Drug Library Mini | FDA-Approved Drug Library | Anti-Cancer Compound Library | metabolism/Protease Compound Library | Drug Repurposing Compound Library Plus | Bioactive Compound Library Plus | Ivosidenib | AGI-5198 | Vorasidenib | AGI-6780 | GSK864 | IDH-305 | BAY-1436032 | Enasidenib mesylate | Mutant IDH1 inhibitor | Mutant IDH1-IN-1 | Mutant IDH1-IN-2 | IDH1 Inhibitor 1 | Mutant IDH1-IN-4 | Olutasidenib

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