中文名:Tucidinostat (Chidamide)
英文名:Tucidinostat (Chidamide)
英文别名:HBI-8000, CS-055;Benzamide, N-(2-amino-4-fluorophenyl)-4-[[[(2E)-1-oxo-3-(3-pyridinyl)-2-propen-1-yl]amino]methyl]-
纯度:10mM in DMSO
货号:T409118
包装:1ml
Cas号:1616493-44-7
存储温度:-80℃储存
产品介绍:
Information
Tucidinostat (Chidamide, HBI-8000, CS-055) is a low nanomolar inhibitor ofHDAC1, 2, 3, and 10, the HDAC isotypes well documented to be associated with the malignant phenotype with IC50 values of 95, 160, 67, 78 nM for HDAC1, 2, 3, 10 respectively.
In vitro
Chidamide inhibits class I HDACs 1-3, as well as class IIb HDAC10, at low nanomolar concentrations. Chidamide significantly induces histone H3 acetylation in both HeLa human cervical adenocarcinoma cells and human PBMC. Cell growth inhibition studies performed with 18 human-derived tumor cell lines demonstrate that chidamide and MS-275 similarly inhibit the in vitro growth of most, but not all, tumor cells in the low micromolar concentration range. However, chidamide, and to a lesser extent MS-275, is significantly less toxic to normal cells from human fetal kidney (CCC-HEK) and liver (CCC-HEL), indicating a differential cytotoxic response of normal cells versus cancerous cells to chidamide.
In vivo
In HCT-8 colorectal carcinoma mice xenografts, Chidamide shows in vivo antitumor activity. Chidamide in the dose range of 12.5-50 mg/kg dose-dependently reduces tumor size and tumor weight, and the dose of 50 mg/kg produces similar or greater efficacy compared with the control drugs 5-fluorouracil(5-FU, 20 mg/kg) and MS-275 (25 mg/kg, which was reported as the maximum tolerated dose in xenograft models). However, chidamide is well-tolerated at the above doses in the tumor-bearing animals, whereas the control drugs cause significant weight loss.
Cell Data
cell lines:
Concentrations:0-400 nM
Incubation Time:0-400 nM
Powder Purity:≥98%
查看阿拉丁官网此产品相关对应页面:https://www.aladdin-e.com/zh_cn/T409118.html
关键字: HBI-8000, CS-055;Benzamide, N-?(2-?amino-?4-?fluorophenyl)?-?4-?[[[(2E)-1-?oxo-?3-?(3-?pyridinyl)?-?2-?propen-?1-?yl]?amino]?methyl]?-
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(www.aladdin-e.com)和海外(www.aladdinsci.com)电商平台。