| Name | Enasidenib mesylate |
| Description | Enasidenib mesylate (AG-221 mesylate) is a potent and selective IDH2 mutase inhibitor that promotes differentiation of leukemia myeloid cells for the treatment of acute myeloid leukemia. |
| In vitro | Reversing the effects of mutant IDH2 on DNA methylation in mutant stem/progenitor cells, Enasidenib mesylate (AG-221) induces differentiation and impairs self-renewal of IDH2-mutant leukemia cells. Simultaneous inhibition of Flt3ITD further enhances these effects. In the context of Enasidenib mesylate (AG-221) therapy, leukemic cells undergo differentiation, resulting in an increased CD11b+ population and a decreased c-Kit+ population in the peripheral blood at 2 weeks[2]. |
| In vivo | In an IDH2-mutant acute myeloid leukemia (AML) primary xenograft mouse model, treatment with Enasidenib mesylate (AG-221) significantly improves survival[1]. Acting as a mutant IDH2 inhibitor, enasidenib remodels the epigenetic state of IDH2-mutant cells, inducing alterations in self-renewal/differentiation in an IDH2-mutant AML model in vivo. Enasidenib mesylate treatment at doses of 10 mg/kg or 100 mg/kg bid results in a substantial reduction in 2-HG levels in vivo, reaching 96.7% below pre-treatment levels.Furthermore, Enasidenib mesylate treatment restores megakaryocyte-erythroid progenitor (MEP) differentiation, which is suppressed by mutant IDH2 expression, as indicated by a mean MEP% increase from 39% in the vehicle group to 50% in the AG-221 group. The therapy also reverses the effects of mutant IDH2 on DNA methylation, with a significant reduction observed in DNA methylation, affecting 180 genes with 20 or more hypomethylated differentially methylated cytosines (DMCs) following treatment.Enasidenib mesylate therapy, particularly at a dose of 100 mg/kg bid, applied to mice engrafted with Mx1-Cre IDH2R140QFlt3ITD AML cells, markedly reduces 2-hydroxyglutarate (2-HG) levels, consistent with on-target inhibition. Enasidenib effectively inhibits the production of 2-HG mediated by mutant IDH2[2]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 80 mg/mL (140.48 mM), Sonication is recommended.
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| Keywords | IDH2 | Enasidenib Mesylate | Enasidenib mesylate | AG-221 Mesylate | AG221 Mesylate | AG 221 Mesylate |
| Inhibitors Related | Disulfiram | 1-Methoxy-4-propylbenzene | Methotrexate | Mycophenolate Mofetil | 18β-Glycyrrhetinic acid | Ribavirin | Methotrexate disodium | 2-Methylaminoethanol | Benzyl alcohol | 2-Bromoacetamide | Isomalt | Sodium Oxamate |
| Related Compound Libraries | Failed Clinical Trials Compound Library | Bioactive Compound Library | Hematonosis Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | FDA-Approved Drug Library | Anti-Cancer Approved Drug Library | Orally Active Compound Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library | Anti-Cancer Drug Library |
United States
