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

Enasidenib mesylate (Synonyms: AG-221 mesylate)

Cat. No.: HY-18690A Purity: 99.25%
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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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 113 In-stock
Estimated Time of Arrival: December 31
5 mg USD 90 In-stock
Estimated Time of Arrival: December 31
10 mg USD 132 In-stock
Estimated Time of Arrival: December 31
50 mg USD 396 In-stock
Estimated Time of Arrival: December 31
100 mg USD 624 In-stock
Estimated Time of Arrival: December 31
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Other Forms of Enasidenib mesylate:

    Enasidenib mesylate purchased from MCE. Usage Cited in: Sci Rep. 2017 Oct 6;7(1):12758.

    Represented western blot of an isothermal dose-response at melting temperature of 59°C demonstrating cellular mIDH1 enzyme thermal stabilization with mIDH1 inhibitors.
    • Biological Activity

    • Technical Information

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    • References

    Description

    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
    Solvent & Solubility
    In Vitro: 

    10 mM in DMSO

    Preparing
    Stock Solutions
    Concentration Solvent 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.
    References
    Molecular Weight

    569.48

    Formula

    C₂₀H₂₁F₆N₇O₄S

    CAS No.

    1650550-25-6

    SMILES

    CS(=O)(O)=O.CC(O)(C)CNC1=NC(C2=NC(C(F)(F)F)=CC=C2)=NC(NC3=CC(C(F)(F)F)=NC=C3)=N1

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

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    Product Name:
    Enasidenib mesylate
    Cat. No.:
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    Enasidenib mesylate

    Cat. No.: HY-18690A