Enasidenib (AG-221)

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

Enasidenib (AG-221) Chemical Structure

Enasidenib (AG-221) Chemical Structure

CAS: 1446502-11-9

Selleck's Enasidenib (AG-221) has been cited by 13 publications

Purity & Quality Control

Batch: Purity: 99.99%
99.99

Enasidenib (AG-221) Related Products

Choose Selective Dehydrogenase Inhibitors

Biological Activity

Description Enasidenib (AG-221) is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzyme.
Targets
IDH2 [1]
(Cell-free assay)
12 nM
In vitro
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].

Cell Research Cell lines OE19 cells
Concentrations 5 μM
Incubation Time 24 h
Method

Cells were treated with different concentrations of Enasidenib.

In Vivo
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 Animal Models Murine models of IDH2-mutant leukemia
Dosages 10 mg/kg or 100 mg/kg bid
Administration --
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04955938 Recruiting
IDH Mutation|IDH1 Mutation|IDH2 Gene Mutation|Blood Cancer|Myeloproliferative Neoplasm
University of Chicago
October 29 2021 Phase 1
NCT03515512 Completed
Acute Myeloid Leukemia|Chronic Myelomonocytic Leukemia
Massachusetts General Hospital|Celgene
July 17 2018 Phase 1
NCT02273739 Completed
Solid Tumor|Glioma|Angioimmunoblastic T-cell Lymphoma|Intrahepatic Cholangiocarcinoma|Chondrosarcoma
Celgene|Celgene Corporation
December 8 2014 Phase 1|Phase 2
NCT02218346 Completed
Healthy Volunteers
Agios Pharmaceuticals Inc.|Celgene Corporation
August 2014 Phase 1

Chemical Information & Solubility

Molecular Weight 473.38 Formula

C19H17F6N7O

CAS No. 1446502-11-9 SDF Download Enasidenib (AG-221) SDF
Smiles CC(C)(CNC1=NC(=NC(=N1)C2=NC(=CC=C2)C(F)(F)F)NC3=CC(=NC=C3)C(F)(F)F)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 94 mg/mL ( (198.57 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 94 mg/mL

Water : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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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
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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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