2. Metabolic Enzyme/Protease
  3. Isocitrate Dehydrogenase (IDH)
  4. Enasidenib

Enasidenib is an oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes, with IC50s of 100 and 400 nM against IDH2R140Q and IDH2R172K, respectively.

For research use only. We do not sell to patients.

CAS No. : 1446502-11-9

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10 mM * 1 mL in DMSO
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Customer Review

Based on 16 publication(s) in Google Scholar

Other Forms of Enasidenib:

Enasidenib Related Antibodies

Top Publications Citing Use of Products

    Enasidenib purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2024 Jul 8:177:117071.  [Abstract]

    Enasidenib (5, 10, and 20 µM) inhibited cell growth in the random sequence group, IDH2wt group, IDH2 R140Q group, and IDH2 R172K group, respectively. The inhibition rate was detected and analyzed using the MTT assay.

    Enasidenib purchased from MedChemExpress. Usage Cited in: Oncogene. 2023 Apr;42(16):1272-1281.  [Abstract]

    Representative SBB staining in the double mutant and WT embryos following in vivo treatment of vehicle control, Gilteritinib, Quizartinib, and Enasidenib at 0.01 μM, 0.1 μM and 1 μM respectively.

    Enasidenib purchased from MedChemExpress. Usage Cited in: bioRxiv. 2023 Sep 12.

    After treating wild-type and mutant IDH chondrosarcoma cell lines with increasing concentrations of Enasidenib for 72 hours, cell viability was measured (WST-1 assay).

    Enasidenib purchased from MedChemExpress. Usage Cited in: bioRxiv. 2023 Sep 12.

    Treatment was administered either with the solvent (control group) or 35 mg/kg Enasidenib twice daily for 21 days. The mean relative tumor volume curve for T-CDS17 xenografts was recorded during treatment.

    Enasidenib purchased from MedChemExpress. Usage Cited in: Cell Rep. 2022 Feb 15;38(7):110391.  [Abstract]

    Enasidenib (10 μM). Gene expression and α-KG content of IDH 1/2 (Idh1/2) in activated macrophages.

    View All Isocitrate Dehydrogenase (IDH) Isoform Specific Products:

    View All Isoforms
    IDH1 IDH2

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Enasidenib is an oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes, with IC50s of 100 and 400 nM against IDH2R140Q and IDH2R172K, respectively.

    IC50 & Target

    IDH2

     

    Cellular Effect
    Cell Line Type Value Description References
    Sf9 IC50
    0.009 μM
    Compound: IDHIFA; AG-221
    Inhibition of full-length C-terminal His6 tagged IDH2 R140Q mutant (1 to 452 residues) (unknown origin) homodimer expressed in Sf9 cells assessed as reduction in NADPH consumption using alpha-ketoglutarate as substrate preincubated for 16 hrs followed by substrate addition and measured after 1 hr by Diaphorase/Resazurin dye based fluorescence assay
    Inhibition of full-length C-terminal His6 tagged IDH2 R140Q mutant (1 to 452 residues) (unknown origin) homodimer expressed in Sf9 cells assessed as reduction in NADPH consumption using alpha-ketoglutarate as substrate preincubated for 16 hrs followed by substrate addition and measured after 1 hr by Diaphorase/Resazurin dye based fluorescence assay
    		[PMID: 32071674]
    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Enasidenib Related Antibodies
    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    473.38

    Formula

    C19H17F6N7O
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

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

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (105.62 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

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    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      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

      This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    • Protocol 2

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

      Solubility: ≥ 1.25 mg/mL (2.64 mM); Clear solution

      This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.93%

    SDS (393 KB)

    COA (250 KB) RP-HPLC (223 KB) MS (68 KB)

    Handling Instructions (2659 KB)
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.1125 mL 10.5623 mL 21.1247 mL 52.8117 mL
    5 mM 0.4225 mL 2.1125 mL 4.2249 mL 10.5623 mL
    10 mM 0.2112 mL 1.0562 mL 2.1125 mL 5.2812 mL
    15 mM 0.1408 mL 0.7042 mL 1.4083 mL 3.5208 mL
    20 mM 0.1056 mL 0.5281 mL 1.0562 mL 2.6406 mL
    25 mM 0.0845 mL 0.4225 mL 0.8450 mL 2.1125 mL
    30 mM 0.0704 mL 0.3521 mL 0.7042 mL 1.7604 mL
    40 mM 0.0528 mL 0.2641 mL 0.5281 mL 1.3203 mL
    50 mM 0.0422 mL 0.2112 mL 0.4225 mL 1.0562 mL
    60 mM 0.0352 mL 0.1760 mL 0.3521 mL 0.8802 mL
    80 mM 0.0264 mL 0.1320 mL 0.2641 mL 0.6601 mL
    100 mM 0.0211 mL 0.1056 mL 0.2112 mL 0.5281 mL
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    Enasidenib Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Enasidenib1446502-11-9AG-221AG221AG 221Isocitrate Dehydrogenase (IDH)Inhibitorinhibitorinhibit

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