产品
编 号：F527194
分子式：C24H29N5O
分子量：403.52
分子式：C24H29N5O
分子量：403.52
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
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5mg
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10mg
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50mg
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结构图
CAS No: 934828-12-3
产品详情
生物活性：
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.
体内研究：
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.
体外研究：
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.
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.
体内研究：
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.
体外研究：
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.
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