计算溶液所需的质量、体积或浓度。
为什么选择此级别
，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
2-8°C储存,干燥。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
EPZ-011989 trifluoroacetate is a potent and orally active Zeste Homolog 2 (EZH2) inhibitor with metabolic stability. EPZ-011989 trifluoroacetate has inhibitory inhibition for EZH2 with a K i value of <3 nM. EPZ-011989 trifluoroacetate shows robust methyl mark inhibition and anti-tumor activity. EPZ-011989 trifluoroacetate can be used for the research of various cancers
In Vitro
EPZ-011989 trifluoroacetate inhibits mutant and wild-type EZH2 with an K i value of <3 nM. EPZ-011989 trifluoroacetate reduces cellular H3K27 methylation with an IC 50 value of 94 nM. EPZ-011989 trifluoroacetate (0-10 μM; 11 days) has anti-proliferation effect in WSU-DLCL2 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: WSU-DLCL2 cells Concentration: 0-10 μM Incubation Time: 11 days Result: Demonstrated an average lowest cytotoxic concentration (LCC) in WSU-DLCL2 cells of 208 nM.
In Vivo
EPZ-011989 trifluoroacetate (oral; 30-1000 mg/kg; single or bid; for 7 days or 21 days) can elicit robust methyl mark inhibition and antitumor activity . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: SCID mice Dosage: 125, 250, 500, and 1000 mg/kg Administration: Oral; single, twice-daily (BID)for 7 days or twice-daily (BID)for 21 days Result: Provided coverage over the LCC for 24 h (1000 mg/kg ), while the 250 and 500 mg/kg doses provided coverage over this value for approximately 8 h. Observed complete ablation of the methyl mark by the end of day 7. Showed robust tumor growth inhibition, methyl mark reduction and extended total and free plasma exposure time. Animal Model: Rat Dosage: 30, 100, and 300 mg/kg Administration: Oral, single Result: dose (mg/kg) route t 1/2 (h) t max (h) C max (ng/mL) AUC inf (h*ng/mL) time above LCC (h) 30 p.o. 4.7 2 240 970 4 100 p.o. 3.9 2.7 1600 5600 8 300 p.o. 3.7 2.7 2900 10000 10
Form:Solid
IC50& Target:EZH2
规格
别名
EPZ011989 三氟乙酸盐
英文名称
EPZ011989 trifluoroacetate
生化机理
EPZ-011989 三氟乙酸盐是一种具有代谢稳定性的强效口服活性 Zeste 同源体 2 (EZH2) 抑制剂。EPZ-011989 三氟乙酸盐对 EZH2 具有抑制作用，其 K i 值小于 3 nM。EPZ-011989 三氟乙酸盐对 EZH2 有很强的甲基化抑制作用。
储存条件
2-8°C储存,干燥
运输条件
低温运输
作用类型
抑制剂
名称和识别符
分子类型
小分子
IUPAC Name
N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-3-[ethyl-[4-[2-methoxyethyl(methyl)amino]cyclohexyl]amino]-2-methyl-5-(3-morpholin-4-ylprop-1-ynyl)benzamide;2,2,2-trifluoroacetic acid
INCHI
1S/C35H51N5O4.C2HF3O2/c1-7-40(30-12-10-29(11-13-30)38(5)15-18-43-6)33-23-28(9-8-14-39-16-19-44-20-17-39)22-31(27(33)4)34(41)36-24-32-25(2)21-26(3)37-35(32)42;3-2(4,5)1(6)7/h21-23,29-30H,7,10-20,24H2,1-6H3,(H,36,41)(H,37,42);(H,6,7)
InChi Key
JAUQBEFSKUVFDO-UHFFFAOYSA-N
Smiles
CCN(C1CCC(CC1)N(C)CCOC)C2=CC(=CC(=C2C)C(=O)NCC3=C(C=C(NC3=O)C)C)C#CCN4CCOCC4.C(=O)(C(F)(F)F)O
PubChem CID
分子量
719.83
技术文档
高级数据
三维结构
交互式化学结构模型
化学和物理性质
溶解性
DMSO : 100 mg/mL (138.92 mM; Need ultrasonic)
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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