Enasidenib (AG-221)

Catalog No.S8205

For research use only.

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

Enasidenib (AG-221) Chemical Structure

CAS No. 1446502-11-9

Selleck's Enasidenib (AG-221) has been cited by 7 Publications

Purity & Quality Control

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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].

Protocol (from reference)

Animal Research:

[1]

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

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 473.38
Formula

C19H17F6N7O

CAS No. 1446502-11-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)(CNC1=NC(=NC(=N1)C2=NC(=CC=C2)C(F)(F)F)NC3=CC(=NC=C3)C(F)(F)F)O

In vivo Formulation Calculator (Clear solution)

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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.

Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04955938 Recruiting Drug: Ivosidenib|Drug: Enasidenib|Drug: Fedratinib IDH Mutation|IDH1 Mutation|IDH2 Gene Mutation|Blood Cancer|Myeloproliferative Neoplasm University of Chicago October 29 2021 Phase 1
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 Active not recruiting Drug: Enasidenib Acute Myeloid Leukemia|Chronic Myelomonocytic Leukemia Massachusetts General Hospital|Celgene July 17 2018 Phase 1
NCT02273739 Completed Drug: Enasidenib Solid Tumor|Glioma|Angioimmunoblastic T-cell Lymphoma|Intrahepatic Cholangiocarcinoma|Chondrosarcoma Celgene|Celgene Corporation December 8 2014 Phase 1|Phase 2
NCT02218346 Completed Drug: AG221 Healthy Volunteers Agios Pharmaceuticals Inc.|Celgene Corporation August 2014 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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