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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 (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.
相关产品:Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Cell Cycle/DNA Damage Compound Library | Epigenetics Compound Library | Histone Modification Research Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Anti-Aging Compound Library | Drug Repurposing Compound Library | Reprogramming Compound Library | Oxygen Sensing Compound Library | Anti-COVID-19 Compound Library | Orally Active Compound Library | Anti-Breast Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Anti-Blood Cancer Compound Library | Anti-Liver Cancer Compound Library | Anti-Pulmonary Fibrosis Compound Library | Osteogenesis Compound Library | Heterocyclic Compound Library | Highly Selective Inhibitors Library | YF479 | KD 5170 | HDAC-IN-48 | Remetinostat | HDAC-IN-30 | HDAC-IN-52 | CG347B | Psammaplin A | JPS016 | HDAC6-IN-9 | Splitomicin | TNG260 | Tacedinaline | G4/HDAC-IN-1 | HPOB | Tubacin | HDAC-IN-37 | Vorinostat-d5 | Resminostat | MAO A/HDAC-IN-1 | NCC-149 | Tubulin/HDAC-IN-1 | PI3K/HDAC-IN-1 | HDAC1-IN-4 | HDAC6/HSP90-IN-1 | Entinostat-d4 | UF010 | MOCPAC | Ivaltinostat | HDAC-IN-56
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货号: HY-100748
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