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

Enasidenib mesylate  (Synonyms: AG-221 mesylate)

Cat. No.: HY-18690A Purity: 99.68%
COA
SDS
Handling Instructions Technical Support

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.

CAS No. : 1650550-25-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 16 publication(s) in Google Scholar

Other Forms of Enasidenib mesylate:

Enasidenib mesylate Related Antibodies

Top Publications Citing Use of Products

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

    IC50 & Target

    IDH2

     

    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].

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

    Enasidenib mesylate 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 (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].

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

    569.48

    Formula

    C20H21F6N7O4S
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    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
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (175.60 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    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
    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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    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

    ×
    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    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (4.39 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (4.39 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    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).

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    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
    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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.7560 mL 8.7799 mL 17.5599 mL 43.8997 mL
    5 mM 0.3512 mL 1.7560 mL 3.5120 mL 8.7799 mL
    10 mM 0.1756 mL 0.8780 mL 1.7560 mL 4.3900 mL
    15 mM 0.1171 mL 0.5853 mL 1.1707 mL 2.9266 mL
    20 mM 0.0878 mL 0.4390 mL 0.8780 mL 2.1950 mL
    25 mM 0.0702 mL 0.3512 mL 0.7024 mL 1.7560 mL
    30 mM 0.0585 mL 0.2927 mL 0.5853 mL 1.4633 mL
    40 mM 0.0439 mL 0.2195 mL 0.4390 mL 1.0975 mL
    50 mM 0.0351 mL 0.1756 mL 0.3512 mL 0.8780 mL
    60 mM 0.0293 mL 0.1463 mL 0.2927 mL 0.7317 mL
    80 mM 0.0219 mL 0.1097 mL 0.2195 mL 0.5487 mL
    100 mM 0.0176 mL 0.0878 mL 0.1756 mL 0.4390 mL
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.

    Enasidenib mesylate 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:

    Enasidenib1650550-25-6AG-221AG221AG 221Isocitrate Dehydrogenase (IDH)Inhibitorinhibitorinhibit

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Requested Quantity *

    Applicant Name *

    		 

    Salutation

    Email Address *

    		 

    Phone Number *

    Department

    		 

    Organization Name *

    City

    State

    Country or Region *

    		      

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    Enasidenib mesylate
    Cat. No.:
    HY-18690A
    Quantity:
    MCE Japan Authorized Agent:

    Customer Review

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Lot #

    Applicant Name *

    		 

    Email Address *

    Phone Number

    		 

    Department *

    Organization Name *

    		 

    Country or Region *

    Remarks

    SAFETY DATA SHEET (SDS)

    English - EN (393 KB) Français - FR (393 KB) Deutsch - DE (393 KB) Norwegian - NO (393 KB) Español - ES (393 KB) Swedish - SV (393 KB) Italian - IT (393 KB) Korean - KR (393 KB) Portuguese - PT (393 KB)

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.