公告提醒:爱必信所有产品和服务仅用于科学研究,不用于临床应用及其他用途提供产品和服务(也不为任何个人提供产品和服务)!

抑制剂描述:

产品名称:Tucidinostat(Chidamide)

产品别名:见爱必信官网

英文别名:Tucidinostat(Chidamide)

靶点:HDAC

CAS:1616493-44-7

纯度:>98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

Chidamide is a low nanomolar inhibitor of HDAC1, 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. 

溶解性:DMSO : ≥ 50 mg/mL (128.07 mM)

体外研究:

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.

体内研究: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.

产品信息订购:

产品更多信息请进入爱必信网站咨询