| 常用名 | EPZ011989 | CAS号 | 1598383-40-4 |
|---|---|---|---|
| 价格 | ¥需询单/25g ¥需询单/5g | 纯度 | 98.0% |
| 备货期 | 需询单 | 库存 | 询单 |
| 产品详情(用途,包装等)
用途: EPZ011989 is a potent, selective orally bioavailable EZH2 inhibitor with Ki 3000-fold selectivity over other HMTase.IC50 value: 15-fold selectivity over EZH1 and >3000-fold selectivity relative to the Ki of 20 other histone methyltransferases (HMTs) tested. EPZ011989 also exhibits metabolic stability. Furthermore, EPZ011989 reduces cellular H3K27 methylation in the Y641F, mutant-bearing human lymphoma cell line, WSU-DLCL2, with an IC50 below 100 nM. This functional response translates to activity in a long-term proliferation assay where EPZ011989 demonstrates an average lowest cytotoxic concentration (LCC) in WSU-DLCL2 cells of 208 nM. In vivo: The LCC parameter, when corrected for plasma protein-binding, predicts an efficacious plasma level in mouse for EPZ011989 of 158 ng/mL. The pharmacokinetics in SCID mice following oral administration of 125, 250, 500, and 1000 mg/kg indicated that the 1000 mg/kg dose provided coverage over the LCC for 24 h, while the 250 and 500 mg/kg doses provided coverage over this value for approximately 8 h. EPZ011989 demonstrates significant tumor growth inhibition in a mouse xenograft model of human B cell lymphoma. 物理化学性质: CAS号:1598383-40-4 常用中文名:EPZ011989 常用英文名:EPZ011989 分子式:C35H51N5O4 分子量:605.810 密度:1.2±0.1 g/cm3 沸点:756.7±60.0 °C at 760 mmHg 熔点:N/A 闪点:411.4±32.9 °C 储存条件:-20℃ |