Home Metabolism Dehydrogenase inhibitor Enasidenib(AG-221) Mesylate For research use only.

Enasidenib(AG-221) Mesylate

Enasidenib (AG-221) mesylate is an orally available, selective and potent inhibitor of mutant isocitrate dehydrogenase 2 (IDH2).

Enasidenib(AG-221) Mesylate Chemical Structure

Enasidenib(AG-221) Mesylate Chemical Structure

CAS No. 1650550-25-6

Purity & Quality Control

Enasidenib(AG-221) Mesylate Related Products

Signaling Pathway

Dehydrogenase Signaling Pathways

Dehydrogenase Signaling Pathway

Biological Activity

Description Enasidenib (AG-221) mesylate is an orally available, selective and potent inhibitor of mutant isocitrate dehydrogenase 2 (IDH2).
Targets
IDH2 [1]
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.[3]
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.[3] 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.[2]
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 569.48 Formula

C20H21F6N7O4S
CAS No. 1650550-25-6 SDF --
Smiles CC(C)(O)CNC1=NC(=NC(=N1)C2=NC(=CC=C2)C(F)(F)F)NC3=CC(=NC=C3)C(F)(F)F.C[S](O)(=O)=O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (175.59 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 10 mg/mL

Water : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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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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