Name: AG-221 (Enasidenib)
Brand: Selleck Chemicals
SKU: S8205
Availability: InStock
Rating: 5 (17 reviews)

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Quality Control

Batch: Purity: 99.99%

99.99

Related Targets	HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism Casein Kinase
Other Dehydrogenase Inhibitors	Vorasidenib (AG-881) (R)-GNE-140 CPI-613 (Devimistat) Glycyrrhizin (Glycyrrhizic Acid, NSC 167409) Sodium Dichloroacetate (DCA) AGI-6780 Emodin Gossypol Acetate AGI-5198 Brequinar (DUP785)

Solubility

In vitro
Batch:

DMSO : 94 mg/mL (198.57 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 94 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (10.56mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (10.56mM)
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	473.38	Formula	C₁₉H₁₇F₆N₇O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1446502-11-9	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			SMILES	CC(C)(CNC1=NC(=NC(=N1)C2=NC(=CC=C2)C(F)(F)F)NC3=CC(=NC=C3)C(F)(F)F)O

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC₅₀/Ki	IDH2 (Cell-free assay) 12 nM
In vitro	Enasidenib (AG-221) has been demonstrated to reduce 2-HG levels by >90% and reverse histone and deoxyribonucleic acid (DNA) hypermethylation in vitro, and to induce differentiation in leukemia cell models.
In vivo	Enasidenib (AG-221) is able to potently reduce 2HG found in the bone marrow, plasma and urine of engrafted mice. Treatment with this compound also induced a dose dependent, statistically significant, survival benefit. A proliferative burst of the human specific CD45+ blast cells is followed by cellular differentiation as measured by the expression of CD11b, CD14 and CD15 and cell morphology after its administration. It also restores megakaryocyte-erythroid progenitor (MEP) differentiation that is suppressed by mutant IDH2 expression and reverses the effects of mutant IDH2 on DNA methylation in mutant stem/progenitor cells. Clinical trials combining IDH2 inhibitors with other targeted AML therapies are warranted in order to increase therapeutic efficacy.
References	[1] http://www.bloodjournal.org/content/124/21/437 [2] http://cancerres.aacrjournals.org/content/74/19_Supplement/3116 [3] https://pubmed.ncbi.nlm.nih.gov/36153371/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-09-03)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03013998	RECRUITING	Previously Untreated Relapsed Refractory Acute Myeloid Leukemia	Beat AML, LLC	2016-11	PHASE2; PHASE3
NCT02813135	RECRUITING	Pediatric Cancer	Gustave Roussy, Cancer Campus, Grand Paris	2016-08-03	PHASE1; PHASE2
NCT05564390	RECRUITING	Acute Myeloid Leukemia; Acute Myeloid Leukemia Arising From Previous Myelodysplastic/Myeloproliferative Neoplasm; Acute Myeloid Leukemia Post Cytotoxic Therapy; Acute Myeloid Leukemia, Myelodysplasia-Related; Myelodysplastic Syndrome	National Cancer Institute (NCI)	2024-06-18	PHASE2
NCT06240754	RECRUITING	Clonal Cytopenia of Undetermined Significance; CCUS Clonal Cytopenia of Undetermined Significance	Washington University School of Medicine	2024-10-10	PHASE2
NCT06176989	RECRUITING	Metastatic Chondrosarcoma; Locally Advanced Chondrosarcoma; Metastatic Sinonasal Adenocarcinoma; Locally Advanced Sinonasal Adenocarcinoma; Metastatic Large-cell Neuroendocrine Carcinoma; Locally Advanced Large-cell Neuroendocrine Carcinoma; Metastatic Olfactory Neuroblastoma; Locally Advanced Olfactory Neuroblastoma; Metastatic Sinonasal Undifferentiated Carcinoma; Locally Advanced Sinonasal Undifferentiated Carcinoma	National Cancer Institute (NCI)	2024-03-04	PHASE2
NCT06756308	ACTIVE_NOT_RECRUITING	T-cell Lymphoma	Memorial Sloan Kettering Cancer Center	2024-12-24	PHASE2

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AG-221 (Enasidenib) Mutant IDH2 Inhibitor

Chemical Structure

Molecular Weight: 473.38