Cat. No.: HY-18690

Enasidenib

(Synonyms: AG-221)

17 Cited Publications

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Based on 17 publication(s) in Google Scholar

Enasidenib is an oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes, with IC₅₀s of 100 and 400 nM against IDH2^R140Q and IDH2^R172K, respectively.

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Pureté: 99.93%
CAS No.: 1446502-11-9
Formule: C₁₉H₁₇F₆N₇O
Masse moléculaire:473.38

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Enasidenib Chemical Structure

CAS No.: 1446502-11-9

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (17)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Enasidenib is an oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes, with IC₅₀s of 100 and 400 nM against IDH2^R140Q and IDH2^R172K, respectively.

IC₅₀ & Target

IDH2

Voir tous les produits spécifiques à Isoform Isocitrate Dehydrogenase (IDH) :

IDH1
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 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	[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 Flt3^ITD. 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.

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 IDH2^R140QFlt3^ITD 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.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1446502-11-9
Appearance Solid
Masse moléculaire 473.38
Formule C₁₉H₁₇F₆N₇O
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
Synonyms

AG-221
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (17)

All Cell Proliferation/Viability AssayCell Imaging/StainingRT-PCRIn Vivo Efficacy Study

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Journal Impact Factor

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 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

Blockage of citrate export prevents TCA cycle fragmentation via Irg1 inactivation. [Abstract]

2022 Feb 15;38(7):110391. PMID: 35172156

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.
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
Res Sq

2026 Jun 15.
Charles University

2026.
Queen Mary University of London

2025.
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 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.
bioRxiv

2023 Sep 12.

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.
Univerzita Karlova v Praz

2021 Jul.

Solvant et solubilité

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

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

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

This protocol yields a clear solution of ≥ 1.25 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 (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during 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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (276 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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Exploring the Pathway: IDH Mutations and Metabolic Dysregulation in Cancer Cells: A Novel Therapeutic Target. MAY 29, 2015

[2]. Alan H. Shih, et al. AG-221, a Small Molecule 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. Blood 2014 124:437.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Enasidenib

17 Cited Publications

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Publications Citing Use of MedChemExpress (MCE) Enasidenib

Voir tous les produits spécifiques à Isoform Isocitrate Dehydrogenase (IDH)

Activité biologique

Chemical Information

Publications (17)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Enasidenib Related Classifications

HY-18690 Related Classifications