EPZ011989 - ≥97% , CAS No.2095432-26-9

CAS: 2095432-26-9 Cat. No.: E413837 Fórmula: C₃₅H₅₁N₅O₄·HCl Peso molecular: 642.27

GRADE & PURITY ≥97%

Synonyms

N-​[(1,​2-​dihydro-​4,​6-​dimethyl-​2-​oxo-​3-​pyridinyl)​methyl]​-​3-​[ethyl[trans-​4-​[(2-​methoxyethyl)​methylamino]​cyclohexyl]​amino]​-​2-​methyl-​5-​[3-​(4-​morpholinyl)​-​1-​propyn-​1-​yl]​-benzamide hydrochloride

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Visão geral

Information

EPZ011989 EPZ011989 is a potent, selective, orally bioavailable EZH2 inhibitor with K i of <3 nM.

Targets

EZH2 (Cell-free assay); EZH1 (Cell-free assay) <3 nM(Ki); 103 nM

In vitro

EPZ011989 equipotently inhibits mutant and wild-type EZH2 with an inhibition constant (Ki) of <3 nM. EPZ011989 is also a specific EZH2 inhibitor with a >15-fold selectivity over EZH1 and >3000-fold selectivity relative to the Ki of 20 other histone methyltransferases (HMTs) tested. As evidenced by the human and rat liver microsomal turnover, EPZ011989 also exhibits metabolic stability. EPZ011989 reduces cellular H3K27 methylation in the Y641F, mutant-bearing human lymphoma cell line, WSU-DLCL2, with an IC50 below 100 nM. EPZ011989 inhibits H3K27me3 in wild-type EZH2 AML cell lines (Kasumi-1, MOLM-13, and MV4-11) at a concentration of 0.625 μM after only four days of treatment. At these concentrations and this time point, no change in viability among these three cell lines is observed and only minimal proliferation inhibition in MV4-11 and MOLM-13 cells.

In vivo

EPZ011989 demonstrates significant tumor growth inhibition in a mouse xenograft model of human B cell lymphoma. EPZ011989 is able to elicit robust methyl mark inhibition and antitumor activity.

Cell Research(from reference)

Cell lines：WSU-DLCL2 cells 

Concentrations：0-10 μM 

Incubation Time：0-11 days 

Specifications

Sinónimos

N-​[(1,​2-​dihydro-​4,​6-​dimethyl-​2-​oxo-​3-​pyridinyl)​methyl]​-​3-​[ethyl[trans-​4-​[(2-​methoxyethyl)​methylamino]​cyclohexyl]​amino]​-​2-​methyl-​5-​[3-​(4-​morpholinyl)​-​1-​propyn-​1-​yl]​-benzamide hydrochloride

Especificações e pureza

≥97%

Mecanismos bioquímicos e fisiológicos

EPZ011989 is a potent, selective, orally bioavailable EZH2 inhibitor with K_i of <3 nM.

Condições de armazenamento de armazenamento

Store at -20°C

Enviado em

Ice chest + Ice pads

Este produto requer transporte de cadeia fria. Serviços terrestres e outros serviços econômicos não estão disponíveis.

Tipo de ação

INHIBITOR

Pureza

≥97%

Nomes e identificadores

• Peso molecular: 642.27

Propriedades químicas e físicas

• Solubilidade: Solubility (25°C) In vitro Ethanol: 100 mg/mL (155.69 mM); DMSO: Insoluble; Water: Insoluble