计算溶液所需的质量、体积或浓度。
为什么选择此级别
提供 ≥97% 纯度，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-20°C储存。超低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
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
规格
英文别名
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
规格或纯度
≥97%
英文名称
EPZ011989
生化机理
EPZ011989 是一种强效、选择性、口服生物利用型 EZH2 抑制剂，其Ki值小于 3 nM。
储存条件
-20°C储存
运输条件
超低温运输
作用类型
抑制剂
纯度
≥97%
名称和识别符
分子类型
小分子
分子量
642.27
技术文档
高级数据
化学和物理性质
溶解性
Solubility (25°C) In vitro Ethanol: 100 mg/mL (155.69 mM); DMSO: Insoluble; Water: Insoluble;
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
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