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Enasidenib(AG-221) Mesylate

Name: Enasidenib(AG-221) Mesylate
Brand: Selleck Chemicals
SKU: S4929
Rating: 5 (3 reviews)

Catalog No.S4929 Purity: 99.90%

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

Enasidenib(AG-221) Mesylate Chemical Structure

CAS: 1650550-25-6

Selleck's Enasidenib(AG-221) Mesylate has been cited by 3 publications

Purity & Quality Control

Batch: S492901 DMSO] 100 mg/mL] false] Ethanol] 10 mg/mL] false] Water] Insoluble] false Purity: 99.90%

99.90

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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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
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

References

Chemical lnformation & 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	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years -20°C powder		1 month-20°Cin solvent

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:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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

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% DMSO + % + % Tween 80 + % ddH₂O

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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.

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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