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[CAS NO. 1446502-11-9] Enasidenib

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Catalog:	HY-18690
Brand:	MCE
CAS:	1446502-11-9

Overview

MDL	MFCD29472245
Molecular Weight	473.38
Molecular Formula	C19H17F6N7O
SMILES	CC(O)(C)CNC1=NC(C2=NC(C(F)(F)F)=CC=C2)=NC(NC3=CC(C(F)(F)F)=NC=C3)=N1

For research use only. We do not sell to patients.

8 Publications Citing Use of MCE

[1]Sci Adv. 2022 Sep 30;8(39):eabq5575.
[2]Nat Commun. 2022 Aug 15;13(1):4785.
[3]Cell Rep. 2022 Feb 15;38(7):110391.
[4]Sci Rep. 2018 Jun 21;8(1):9472.
[5]Sci Rep. 2017 Oct 6;7(1):12758.
[6]ACS Med Chem Lett. 2018 May 1;9(7):606-611.
[7]Spectrochim Acta A Mol Biomol Spectrosc. 22 December 2021, 120790.
[8]Univerzita Karlova v Praz. 2021 Jul.

Summary

Enasidenib is an oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes, with IC ₅₀ s of 100 and 400 nM against IDH2 ^R140Q and IDH2 ^R172K , respectively.

IC50 & Target

IC50: 100 nM (IDH2 ^R140Q ), 400 nM (IDH2 ^R172K ) ^[1]

In Vitro

Enasidenib (AG-221) reverses the effects of mutant IDH2 on DNA methylation in mutant stem/progenitor cells. Enasidenib induces differentiation and impairs self-renewal of IDH2-mutant leukemia cells, effects that are further enhanced by simultaneous inhibition of Flt3 ^ITD . Enasidenib (AG-221) therapy induces differentiation of leukemic cells, with an increase in the CD11b ⁺ population and a decrease in the c-Kit ⁺ population in the peripheral blood at 2wks ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Treatment with Enasidenib (AG-221) significantly improves survival in an IDH2-mutant acute myeloid leukemia (AML) primary xenograft mouse model ^[1] . Enasidenib (AG-221), a mutant IDH2 inhibitor, remodels the epigenetic state of IDH2-mutant cells and induces alterations in self-renewal/differentiation in IDH2-mutant AML model in vivo. Enasidenib treatment (10mg/kg or 100mg/kg bid) leads to a reduction in 2-HG in vivo (96.7% below pre-treatment levels). Moreover, Enasidenib treatment restores megakaryocyte-erythroid progenitor (MEP) differentiation that is suppressed by mutant IDH2 expression (mean MEP% mean, 39% Veh vs 50% AG-221). Enasidenib therapy reverses the effects of mutant IDH2; a significant reduction is observed in DNA methylation, including 180 genes that have 20 or more hypomethylated differentially methylated cytosines (DMCs) following treatment. Enasidenib (100mg/kg bid) treatment of mice engrafted with Mx1-Cre IDH2 ^R140Q Flt3 ^ITD AML cells markedly reduces 2-hydroxyglutarate (2-HG) levels consistent with on target inhibition. Enasidenib inhibits mutant IDH2-mediated 2-HG production ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT03290443	Celgene	Hepatic Impairment	September 21, 2017	Phase 1
NCT03825796	Jonsson Comprehensive Cancer Center\|Jazz Pharmaceuticals	Recurrent Acute Myeloid Leukemia	April 12, 2019	Phase 2
NCT04281498	John Mascarenhas\|Celgene Corporation\|Incyte Corporation\|Myeloproliferative Neoplasms Research Consortium\|National Institutes of Health (NIH)\|National Cancer Institute (NCI)\|Icahn School of Medicine at Mount Sinai	Accelerated+Blast-phase Myeloproliferative Neoplasm\|Chronic-phase Myelofibrosis\|IDH2 Mutation	January 20, 2021	Phase 2
NCT02443168	Celgene	Healthy Volunteers	May 14, 2015	Phase 1
NCT04522895	Heinrich-Heine University, Duesseldorf\|Celgene Corporation\|Koordinierungszentrum für Klinische Studien Düsseldorf	Leukemia, Myeloid, Acute\|Myelodysplastic Syndromes\|Chronic Myelomonocytic Leukemia\|IDH2 Gene Mutation\|IDH2 R172\|IDH2 R140	August 27, 2020	Phase 2
NCT04774393	M.D. Anderson Cancer Center	Acute Myeloid Leukemia\|Recurrent Acute Myeloid Leukemia\|Refractory Acute Myeloid Leukemia	May 24, 2021	Phase 1\|Phase 2
NCT04573582	Celgene	Hepatic Impairment	November 13, 2020	Phase 1
NCT04092179	University Health Network, Toronto\|Celgene\|AbbVie	Acute Myeloid Leukemia\|Relapsed Cancer\|Refractory Cancer\|IDH2 Gene Mutation	November 5, 2020	Phase 1\|Phase 2
NCT02632708	Institut de Recherches Internationales Servier\|Celgene Corporation\|Servier	Newly Diagnosed Acute Myeloid Leukemia (AML)\|Untreated AML\|AML Arising From Myelodysplastic Syndrome (MDS)\|AML Arising From Antecedent Hematologic Disorder (AHD)\|AML Arising After Exposure to Genotoxic Injury	December 31, 2015	Phase 1
NCT04955938	University of Chicago	IDH Mutation\|IDH1 Mutation\|IDH2 Gene Mutation\|Blood Cancer\|Myeloproliferative Neoplasm	October 29, 2021	Phase 1
NCT02218346	Agios Pharmaceuticals, Inc.\|Celgene Corporation	Healthy Volunteers	August 2014	Phase 1
NCT05282459	Tian Yi Zhang\|Celgene Corporation\|Stanford University	Leukemia\|Leukemia, Myeloid\|Monocytic Leukemia	January 12, 2022	Phase 1\|Phase 2
NCT03683433	M.D. Anderson Cancer Center\|National Cancer Institute (NCI)	Acute Bilineal Leukemia\|Acute Biphenotypic Leukemia\|Chronic Myelomonocytic Leukemia\|IDH2 Gene Mutation\|Myelodysplastic Syndrome\|Recurrent Acute Myeloid Leukemia\|Refractory Acute Myeloid Leukemia	September 18, 2018	Phase 2
NCT03383575	M.D. Anderson Cancer Center\|National Cancer Institute (NCI)\|Celgene	Acute Myeloid Leukemia\|Blasts 20-30 Percent of Bone Marrow Nucleated Cells\|Chronic Myelomonocytic Leukemia\|IDH2 Gene Mutation\|Myelodysplastic Syndrome With Excess Blasts\|Recurrent High Risk Myelodysplastic Syndrome\|Refractory High Risk Myelodysplastic Syndrome	January 17, 2018	Phase 2
NCT05401097	Alice Mims\|Ohio State University Comprehensive Cancer Center	Acute Myeloid Leukemia	August 1, 2022	Phase 2
NCT04310527	Celgene	Healthy Volunteers	October 9, 2019	Phase 1
NCT02813135	Gustave Roussy, Cancer Campus, Grand Paris\|National Cancer Institute, France	Children, Adolescents and Young Adults With Refractory or Recurrent Malignancies	August 3, 2016	Phase 1\|Phase 2
NCT02387866	Celgene	Healthy	March 2, 2015	Phase 1
NCT02677922	Celgene	Leukemia, Myeloid, Acute	June 3, 2016	Phase 1\|Phase 2
NCT03744390	Groupe Francophone des Myelodysplasies	Myelodysplastic Syndromes\|Leukemia Acute Myeloid	April 2, 2019	Phase 2
NCT03839771	Stichting Hemato-Oncologie voor Volwassenen Nederland\|Deutsch-Österreichische Studiengruppe Akute Myeloische Leukämie (AMLSG)	Acute Myeloid Leukemia\|Myelodysplastic Syndrome With Excess Blasts-2	March 1, 2019	Phase 3
NCT03728335	City of Hope Medical Center\|National Cancer Institute (NCI)	Acute Myeloid Leukemia	July 11, 2019	Phase 1
NCT02577406	Celgene	Leukemia, Myeloid\|Isocitrate Dehydrogenase	December 30, 2015	Phase 3
NCT03515512	Massachusetts General Hospital\|Celgene	Acute Myeloid Leukemia\|Chronic Myelomonocytic Leukemia	July 17, 2018	Phase 1
NCT04655391	City of Hope Medical Center\|National Cancer Institute (NCI)	Recurrent Acute Myeloid Leukemia	June 25, 2022	Phase 1
NCT05010772	M.D. Anderson Cancer Center\|National Cancer Institute (NCI)	Acute Myeloid Leukemia	October 25, 2021	Phase 1
NCT04203316	Children´s Oncology Group\|National Cancer Institute (NCI)	Recurrent Acute Myeloid Leukemia\|Refractory Acute Myeloid Leukemia	March 30, 2020	Phase 2
NCT02273739	Celgene\|Celgene Corporation	Solid Tumor\|Glioma\|Angioimmunoblastic T-cell Lymphoma\|Intrahepatic Cholangiocarcinoma\|Chondrosarcoma	December 8, 2014	Phase 1\|Phase 2
NCT03720366	Celgene	Leukemia, Myeloid, Acute	December 11, 2018	Phase 1
NCT03013998	Beat AML, LLC	Previously Untreated Acute Myeloid Leukemia	November 2016	Phase 1\|Phase 2
NCT05441514	City of Hope Medical Center\|National Cancer Institute (NCI)	Recurrent Acute Myeloid Leukemia\|Refractory Acute Myeloid Leukemia	November 28, 2022	Phase 1
NCT01915498	Celgene\|Agios Pharmaceuticals, Inc.	Hematologic Neoplasms	August 27, 2013	Phase 1\|Phase 2
NCT03723057	Celgene	Acute Myeloid Leukemia
NCT04075747	Jazz Pharmaceuticals	Acute Myeloid Leukemia	December 2, 2019	Phase 1
NCT03878524	OHSU Knight Cancer Institute\|Oregon Health and Science University	Accelerated Phase Chronic Myelogenous Leukemia, BCR-ABL1 Positive\|Anatomic Stage IV Breast Cancer AJCC v8\|Anemia\|Ann Arbor Stage III Hodgkin Lymphoma\|Ann Arbor Stage III Non-Hodgkin Lymphoma\|Ann Arbor Stage IV Hodgkin Lymphoma\|Ann Arbor Stage IV Non-Hodgkin Lymphoma\|Atypical Chronic Myeloid Leukemia, BCR-ABL1 Negative\|Blast Phase Chronic Myelogenous Leukemia, BCR-ABL1 Positive\|Castration-Resistant Prostate Carcinoma\|Chronic Phase Chronic Myelogenous Leukemia, BCR-ABL1 Positive\|Hematopoietic and Lymphoid System Neoplasm\|Locally Advanced Pancreatic Adenocarcinoma\|Metastatic Breast Carcinoma\|Metastatic Malignant Solid Neoplasm\|Metastatic Pancreatic Adenocarcinoma\|Myelodysplastic+Myeloproliferative Neoplasm With Ring Sideroblasts and Thrombocytosis\|Myelodysplastic+Myeloproliferative Neoplasm, Unclassifiable\|Primary Myelofibrosis\|Recurrent Acute Lymphoblastic Leukemia\|Recurrent Acute Myeloid Leukemia\|Recurrent Chronic Lymphocytic Leukemia\|Recurrent Chronic Myelogenous Leukemia, BCR-ABL1 Positive\|Recurrent Hematologic Malignancy\|Recurrent Hodgkin Lymphoma\|Recurrent Myelodysplastic Syndrome\|Recurrent Myelodysplastic+Myeloproliferative Neoplasm\|Recurrent Myeloproliferative Neoplasm\|Recurrent Non-Hodgkin Lymphoma\|Recurrent Plasma Cell Myeloma\|Recurrent Small Lymphocytic Lymphoma\|Refractory Acute Lymphoblastic Leukemia\|Refractory Acute Myeloid Leukemia\|Refractory Chronic Lymphocytic Leukemia\|Refractory Chronic Myelogenous Leukemia, BCR-ABL1 Positive\|Refractory Chronic Myelomonocytic Leukemia\|Refractory Hematologic Malignancy\|Refractory Hodgkin Lymphoma\|Refractory Malignant Solid Neoplasm\|Refractory Myelodysplastic Syndrome\|Refractory Myelodysplastic+Myeloproliferative Neoplasm\|Refractory Non-Hodgkin Lymphoma\|Refractory Plasma Cell Myeloma\|Refractory Primary Myelofibrosis\|Refractory Small Lymphocytic Lymphoma\|Stage II Pancreatic Cancer AJCC v8\|Stage III Pancreatic Cancer AJCC v8\|Stage IV Pancreatic Cancer AJCC v8\|Stage IV Prostate Cancer AJCC v8\|Unresectable Pancreatic Adenocarcinoma	April 1, 2020	Phase 1
NCT05102370	Memorial Sloan Kettering Cancer Center	Clonal Cytopenia of Undetermined Significance\|CCUS Clonal Cytopenia of Undetermined Significance	October 6, 2021	Phase 1
NCT03881735	Roswell Park Cancer Institute\|Celgene	Blasts Under 5 Percent of Peripheral Blood White Cells\|Bone Marrow Blasts Decreased by 50 Percent or More Compared to Pretreatment Level\|IDH2 Gene Mutation\|Recurrent Acute Myeloid Leukemia\|Refractory Acute Myeloid Leukemia	December 2, 2019	Phase 2

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL ( 105.62 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1125 mL	10.5623 mL	21.1247 mL
5 mM	0.4225 mL	2.1125 mL	4.2249 mL
10 mM	0.2112 mL	1.0562 mL	2.1125 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: 2.08 mg/mL (4.39 mM); Suspended solution; Need ultrasonic and warming
2.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 1.25 mg/mL (2.64 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 1.25 mg/mL (2.64 mM); Clear solution

* All of the co-solvents are available by MCE.

References

[1] Exploring the Pathway: IDH Mutations and Metabolic Dysregulation in Cancer Cells: A Novel Therapeutic Target. MAY 29, 2015
[2] Alan H. Shih, et al. AG-221, a Small Molecule Mutant IDH2 Inhibitor, Remodels the Epigenetic State of IDH2-Mutant Cells and Induces Alterations in Self-Renewal/Differentiation in IDH2-Mutant AML Model in Vivo. Blood 2014 124:437.

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