Enasidenib (AG-221)

For research use only.

Catalog No.S8205

2 publications

Enasidenib (AG-221) Chemical Structure

Molecular Weight(MW): 473.38

Enasidenib (AG-221) is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzyme.

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Biological Activity

Description Enasidenib (AG-221) is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzyme.
In vitro

The compound 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[2].

In vivo

AG-221 is able to potently reduce 2HG found in the bone marrow, plasma and urine of engrafted mice. Treatment 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 AG-221 treatment[2]. AG-221 treatment 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[1].


Animal Research:


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  • Animal Models: Murine models of IDH2-mutant leukemia
  • Dosages: 10 mg/kg or 100 mg/kg bid
  • Administration: --
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 94 mg/mL (198.57 mM)
Ethanol 94 mg/mL (198.57 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 473.38


CAS No. 1446502-11-9
Storage powder
in solvent
Synonyms N/A
Smiles CC(C)(O)CNC1=NC(=NC(=N1)NC2=CC=NC(=C2)C(F)(F)F)C3=NC(=CC=C3)C(F)(F)F

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04203316 Recruiting Drug: Enasidenib|Drug: Enasidenib Mesylate Recurrent Acute Myeloid Leukemia|Refractory Acute Myeloid Leukemia Children''s Oncology Group|National Cancer Institute (NCI) March 30 2020 Phase 2
NCT03515512 Recruiting Drug: Enasidenib Acute Myeloid Leukemia|Chronic Myelomonocytic Leukemia Massachusetts General Hospital|Celgene July 17 2018 Phase 1
NCT02273739 Completed Drug: AG-221 Solid Tumor|Glioma|Angioimmunoblastic T-cell Lymphoma|Intrahepatic Cholangiocarcinoma|Chondrosarcoma Celgene|Celgene Corporation October 24 2014 Phase 1|Phase 2
NCT02218346 Completed Drug: AG221 Healthy Volunteers Agios Pharmaceuticals Inc.|Celgene Corporation August 2014 Phase 1
NCT01915498 Active not recruiting Drug: AG-221 Hematologic Neoplasms Celgene|Agios Pharmaceuticals Inc. August 27 2013 Phase 1|Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID