Enasidenib mesylate
Based on 17 publication(s) in Google Scholar
Enasidenib mesylate is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.68%
- CAS No.: 1650550-25-6
- Formule: C20H21F6N7O4S
- Masse moléculaire:569.48
-
Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Activité biologique
-
Chemical Information
-
Solvant et solubilité
- Pureté et documentation
- Références
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Enasidenib mesylate
More- Cancer Cell. 2025 Dec 21:S1535-6108(25)00502-1. [Abstract]
- Nat Commun. 2022 Aug 15;13(1):4785. [Abstract]
- Sci Adv. 2022 Sep 30;8(39):eabq5575. [Abstract]
- Oncogene. 2023 Apr;42(16):1272-1281. [Abstract]
- Cell Rep. 2022 Feb 15;38(7):110391. [Abstract]
- J Med Chem. 2023 Apr 13;66(7):5279-5288. [Abstract]
- Acta Neuropathol Commun. 2023 Nov 27;11(1):186. [Abstract]
- Sci Rep. 2018 Jun 21;8(1):9472. [Abstract]
- Sci Rep. 2017 Oct 6;7(1):12758. [Abstract]
- Spectrochim Acta A Mol Biomol Spectrosc. 2022 Apr 5:270:120790. [Abstract]
- ACS Med Chem Lett. 2018 May 1;9(7):606-611. [Abstract]
- Res Sq. 2026 Jun 15.
- Charles University. 2026.
- Queen Mary University of London. 2025.
- Biomed Pharmacother. 2024 Aug:177:117071. [Abstract]
- bioRxiv. 2023 Sep 12.
- Univerzita Karlova v Praz. 2021 Jul.
Customer Validation & Images
-
Cell Proliferation/Viability Assay
-
Cell Imaging/Staining
-
Cell Proliferation/Viability Assay
-
In Vivo Efficacy Study
-
RT-PCR
Activité biologique
Description
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.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 1650550-25-6
-
Appearance Solid
-
Masse moléculaire 569.48
-
Formule C20H21F6N7O4S
-
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
-
Synonyms
AG-221 mesylate
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (17)
-
Journal Impact Factor
-
Most Recent
-
Cancer Cell
Tumor-antigen-independent targeting of solid tumors by armored macrophage-directed anti-TREM2 CAR T cells. [Abstract]2025 Dec 21:S1535-6108(25)00502-1. PMID: 41576928 -
Nat Commun
Resistance to the isocitrate dehydrogenase 1 mutant inhibitor ivosidenib can be overcome by alternative dimer-interface binding inhibitors. [Abstract]2022 Aug 15;13(1):4785. PMID: 35970853 -
Sci Adv
Therapeutic implications of mitochondrial stress-induced proteasome inhibitor resistance in multiple myeloma. [Abstract]2022 Sep 30;8(39):eabq5575. PMID: 36170375 -
Oncogene
Transgenic IDH2R172K and IDH2R140Q zebrafish models recapitulated features of human acute myeloid leukemia. [Abstract]2023 Apr;42(16):1272-1281. PMID: 36739363
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.
-
Cell Rep
2022 Feb 15;38(7):110391. PMID: 35172156
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.
-
J Med Chem
Differentiating Inhibition Selectivity and Binding Affinity of Isocitrate Dehydrogenase 1 Variant Inhibitors. [Abstract]2023 Apr 13;66(7):5279-5288. PMID: 36952395 -
Acta Neuropathol Commun
Genetic alterations that deregulate RB and PDGFRA signaling pathways drive tumor progression in IDH2-mutant astrocytoma. [Abstract]2023 Nov 27;11(1):186. PMID: 38012788 -
Sci Rep
A widely-applicable high-throughput cellular thermal shift assay (CETSA) using split Nano Luciferase. [Abstract]2018 Jun 21;8(1):9472. PMID: 29930256 -
Sci Rep
Assessing inhibitors of mutant isocitrate dehydrogenase using a suite of pre-clinical discovery assays. [Abstract]2017 Oct 6;7(1):12758. PMID: 28986582 -
Spectrochim Acta A Mol Biomol Spectrosc
Spectroscopic and computational investigation of the interaction between the new anticancer agent enasidenib and human serum albumin. [Abstract]2022 Apr 5:270:120790. PMID: 34974294 -
ACS Med Chem Lett
Synthesis and Evaluation of a 18F-Labeled Triazinediamine Analogue for Imaging Mutant IDH1 Expression in Gliomas by PET. [Abstract]2018 May 1;9(7):606-611. PMID: 30034587 -
-
-
-
Biomed Pharmacother
A novel iheyamine A derivative L42 suppresses acute myeloid leukemia via dual regulation of the PI3K/AKT/FOXO3a axis and TNF signaling pathway. [Abstract]2024 Aug:177:117071. PMID: 38981243
Enasidenib mesylate purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2024 Aug: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: 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.
-
Solvant et solubilité
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
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).
Working solution concentration: 0.22 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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
-
Fiche technique (278 KB)
-
SDS (393 KB)
- 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)
-
Instruction de manipulation (2659 KB)
Références
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 |
Enasidenib mesylate Related Classifications
HY-18690A Related Classifications
Powered by Bioz