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

Enasidenib (Synonyms: AG-221)

Cat. No.: HY-18690 Purity: 99.95%
Handling Instructions

Enasidenib 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 Chemical Structure

Enasidenib Chemical Structure

CAS No. : 1446502-11-9

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 92 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
5 mg USD 84 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 120 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 348 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg USD 588 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Other Forms of Enasidenib:

    Enasidenib 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

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

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

    IC50 & Target

    IDH2[1]

    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[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 (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[2].

    Clinical Trial
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 83.33 mg/mL (176.03 mM)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1125 mL 10.5623 mL 21.1247 mL
    5 mM 0.4225 mL 2.1125 mL 4.2249 mL
    10 mM 0.2112 mL 1.0562 mL 2.1125 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.08 mg/mL (4.39 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: 2.08 mg/mL (4.39 mM); Suspended solution; Need ultrasonic and warming

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.08 mg/mL (4.39 mM); Clear solution

    References
    Molecular Weight

    473.38

    Formula

    C₁₉H₁₇F₆N₇O

    CAS No.

    1446502-11-9

    SMILES

    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
    Cat. No.:
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    Enasidenib

    Cat. No.: HY-18690