EPZ-011989 trifluoroacetate
更新时间：2024-07-15 12:32:35
采购访问：19次
| 常用名 | EPZ011989三氟乙酸盐 | CAS号 | 1598383-41-5 |
|---|---|---|---|
| 价格 | 纯度 | 98.0% | |
| 备货期 | 10天 | 库存 | 现货 |
| 产品详情（用途，包装等）
用途： EPZ011989 trifluoroacetate 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：1598383-41-5 常用中文名：EPZ011989三氟乙酸盐 常用英文名：EPZ011989 (trifluoroacetate) 分子式：C37H52F3N5O6 分子量：719.834 密度：N/A 沸点：N/A 熔点：N/A 闪点：N/A 储存条件：2-8℃ |
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- 产品名：EPZ-011989 trifluoroacetate
- 价格：
- 纯度：98.0%
- 备货期：10天
- 联系人：徐经理
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参考价格：￥1120/5 mg