Zabadinostat,934828-12-3

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Zabadinostat

CAS No. : 934828-12-3

MCE 国际站：Zabadinostat

产品活性：Zabadinostat (CXD101) 是一种有效的，选择性的，具有口服活性的 I 类 HDAC 抑制剂，对 HDAC1，HDAC2 和 HDAC3 的 IC₅₀ 分别为 63 nM，570 nM 和 550 nM。Zabadinostat 对 II 类 HDAC 没有活性，并具有抗肿瘤活性。

研究领域：Cell Cycle/DNA Damage  |  Epigenetics

作用靶点：HDAC

In Vitro: 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.

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 [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.

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