中文名：西他司他
英文名：Citarinostat (ACY-241)
纯度：Moligand™，≥98%
货号：C414019
Cas号：1316215-12-9
存储温度：-20°C储存
运输条件：超低温运输
产品介绍：
Information
Citarinostat (ACY-241, HDAC-IN-2) is an orally available selectiveHDAC6inhibitor with IC50 of 2.6 nM and 46 nM for HDAC6 and HDAC3, respectively. It has 13 to 18-fold selectivity towards HDAC6 in comparison to HDAC1-3.
Targets
HDAC6 (Cell-free assay); HDAC1 (Cell-free assay); HDAC2 (Cell-free assay); HDAC3 (Cell-free assay); HDAC8 (Cell-free assay) 2.6 nM; 35 nM; 45 nM; 46 nM; 137 nM
In vitro
In cell lines from multiple solid tumor lineages, combination treatment with ACY-241 and paclitaxel enhances inhibition of proliferation and increases cell death relative to either single agent alone. Combination treatment with ACY-241 and paclitaxel also results in more frequent occurrence of mitotic cells with abnormal multipolar spindles and aberrant mitoses, and is associated with increased frequency of abnormal multipolar mitotic spindle formation, induction of aneuploidy, and increased cell death. In A2780 ovarian cancer cells, 24 hour treatment with 300 nM ACY-241 results in increased hyperacetylation of α-tubulin, consistent with inhibition of the tubulin deacetylase HDAC6. Low exposures of ACY-241 result in selective inhibition of HDAC6, while higher exposures lead to inhibition of Class I HDAC isozymes.
In vivo
ACY-241 has a favourable safety profile than non-selective pan-HDAC inhibitors. It has the potential for a substantially reduced side effect profile versus current nonselective HDAC inhibitor drug candidates due to reduced potency against Class I HDACs while retaining the potential for anticancer effectiveness.
Cell Research(from reference)
Cell lines：A2780 ovarian cancer cells
Concentrations：0.1, 0.3, 0.5, 1, 3 μM
Incubation Time：24 h
查看阿拉丁官网此产品相关对应页面：https://www.aladdin-e.com/zh_cn/C414019.html
关键字： CCG-269430 ; Compound (I) [WO2016200919] ; EX-A379 ; HMS2093L12
上海阿拉丁生化科技股份有限公司是A股上市公司（（股票代码：688179），专注于科研试剂的研发、生产和销售，已陆续建立多个工厂和研发中心。作为领军企业，阿拉丁始终坚持质量第一，连续13年被评为“最受欢迎试剂品牌”。
阿拉丁目前常备库存试剂产品品种超过7万种，SKU总数超过46万，产品线涵盖了化学试剂、生化试剂、药靶配体、蛋白质和抗体等多个领域，是国内少数化学试剂到生物试剂全面发展的国产试剂品牌，产品同步发布在我们国内外电商平台。