| 產品描述： | Zabadinostat (CXD101) is a potent, selective and orally active class I HDAC inhibitor with IC50s 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 |
| 靶點： |
HDAC1:63 nM (IC50);HDAC3:550 nM (IC50);HDAC2:570 nM (IC50);HDAC |
| 體外研究： |
Zabadinostat has been tested in vitro in colon, lung, non-Hodgkin lymphoma, and myeloma cell lines with IC50s ranged from 0.2 to 15 μM |
| 體內研究： |
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 (Cmax) are reached 1 to 2 hours after the dose and terminal half‐lives are 6 hours and 8 hours, respectively. After murine oral [14C]-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 |
| 參考文獻： |
1. Eyre TA, et al. Predictive biomarkers for disease sensitivity in lymphoma - the holy grail for HDAC inhibitors? Oncotarget. 2018 Dec 18;9(99):37280-37281. 2. Eyre TA, et al. A phase 1 study to assess the safety, tolerability, and pharmacokinetics of CXD101 in patients with advanced cancer. Cancer. 2019 Jan 1;125(1):99-108. |
| 溶解性： |
Soluble in DMSO |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.478 ml |
12.391 ml |
24.782 ml |
| 5 mM |
0.496 ml |
2.478 ml |
4.956 ml |
| 10 mM |
0.248 ml |
1.239 ml |
2.478 ml |
| 50 mM |
0.05 ml |
0.248 ml |
0.496 ml |
|
| 注意： |
部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。 |
上海工商
危險品化學品經營許可證（不帶存儲）
營業執照(三證合一)
北京