Zabadinostat
规格
| Cas Number | 934828-12-3(DMSO) |
| 规格或纯度 | 10mM in DMSO |
| 包装 | 1ml |
产品信息
| 品牌 | 阿拉丁 |
| 浓度 | 10mM in DMSO |
| 过滤标签 | 表观遗传学,HDAC,Cell Cycle/DNA Damage,Compound libraries |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 生化和生理学机理 | 扎巴地诺司他（CXD101）是一种强效、选择性和口服活性的 I 类 HDAC 抑制剂，对 HDAC1、HDAC2 和 HDAC3 的 IC 50 s 分别为 63 nM、570 nM 和 550 nM。扎巴司他对 HDAC II 类没有活性。扎巴地诺司他（Zabadinostat）对 HDAC1、HDAC2 和 HDAC3 具有抗肿瘤活性。 |
| 英文描述 |
Zabadinostat (CXD101) is a potent, selective and orally active class I HDAC inhibitor with IC 50 s of 63 nM, 570 nM and 550 nM for HDAC1 , HDAC2 and HDAC3 , respectively. Zabadinostat has no activity against HDAC class II. Zabadinostat has antitumor activity In Vitro Zabadinostat has been tested in vitro in colon, lung, non-Hodgkin lymphoma, and myeloma cell lines with IC 50 s ranged from 0.2 to 15 μM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo Zabadinostat substantially reduces tumor size in murine xenograft lung (A549a) and colon (HT29) models at a dose of 50 mg/kg. Tumor reductions are found to be associated with increased histone acetylation and decreased HDAC enzyme activity. For Zabadinostat, after oral dosing in murine and canine models, peak plasma concentrations (C max ) are reached 1 to 2 hours after the dose and terminal half‐lives are 6 hours and 8 hours, respectively. After murine oral [ 14 C]-Zabadinostat at a dose of 1.6 mg/kg (4 μmol/kg), tissue radioactivity peaked 3 to 6 hours after the dose and declined slowly thereafter with Zabadinostat‐related material still present in tissue 21 days after the dose. MCE has not independently confirmed the accuracy of these methods. They are for reference only. IC50& Target:HDAC1 63 nM (IC 50 ) HDAC3 550 nM (IC 50 ) HDAC2 570 nM (IC 50 ) |