Enasidenib (AG-221) - Moligand™, 10mM in DMSO , Inhibitor of isocitrate dehydrogenase (NADP(+)) 2, CAS No.1446502-11-9, Inhibitor of isocitrate dehydrogenase (NADP(+)) 2

CAS: 1446502-11-9 Cat. No.: E407789 Molecular Weight: 473.4 EC Number: 107-597-8

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

2-​Propanol, 2-​methyl-​1-​[[4-​[6-​(trifluoromethyl)​-​2-​pyridinyl]​-​6-​[[2-​(trifluoromethyl)​-​4-​pyridinyl]​amino]​-​1,​3,​5-​triazin-​2-​yl]​amino]​-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Enasidenib (AG-221) 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.

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. 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.
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Synonyms

2-​Propanol, 2-​methyl-​1-​[[4-​[6-​(trifluoromethyl)​-​2-​pyridinyl]​-​6-​[[2-​(trifluoromethyl)​-​4-​pyridinyl]​amino]​-​1, ​3, ​5-​triazin-​2-​yl]​amino]​-

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

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

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

INHIBITOR

Mechanism of action

Inhibitor of isocitrate dehydrogenase (NADP(+)) 2

Names and Identifiers

• Isomeric SMILES: CC(C)(CNC1=NC(=NC(=N1)C2=NC(=CC=C2)C(F)(F)F)NC3=CC(=NC=C3)C(F)(F)F)O
• Molecular Weight: 473.4
• Reaxy-Rn: 23776155
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=23776155&ln=

Associated Targets(Human)

IDH2 Tclin Isocitrate dehydrogenase [NADP], mitochondrial (7 Activities)

Discover Target: IDH2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)