1. Metabolic Enzyme/Protease
  2. Isocitrate Dehydrogenase (IDH)

Enasidenib mesylate (Synonyms: AG-221 mesylate)

Cat. No.: HY-18690A
Handling Instructions

Enasidenib mesylate is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes.

For research use only. We do not sell to patients.
Enasidenib mesylate Chemical Structure

Enasidenib mesylate Chemical Structure

CAS No. : 1650550-25-6

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5 mg USD 90 Get quote
10 mg USD 132 Get quote
50 mg USD 396 Get quote
100 mg USD 624 Get quote

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Enasidenib mesylate is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes.

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 2 wks[2].

In Vivo

Treatment with enasidenib (AG-221) significantly improves survival in an IDH2-mutant acute myeloid leukemia (AML) primary xenograft mouse model[1]. 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 (10 mg/kg or 100 mg/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 (100 mg/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[2].

Clinical Trial
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Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 1.7560 mL 8.7799 mL 17.5599 mL
5 mM 0.3512 mL 1.7560 mL 3.5120 mL
10 mM 0.1756 mL 0.8780 mL 1.7560 mL
Please refer to the solubility information to select the appropriate solvent.
Molecular Weight







Please store the product under the recommended conditions in the Certificate of Analysis.


Room temperature in continental US; may vary elsewhere

Solvent & Solubility


* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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