您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > NCT-501
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
NCT-501
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
NCT-501图片
CAS NO:1802088-50-1
规格:98%
分子量:416.52
包装与价格:
包装价格(元)
5mg电议
25mg电议

产品介绍

Aldehyde Dehydrogenase 1A1 (ALDH1A1) inhibitor, Potent and Selective
CAS:1802088-50-1
分子式:C21H32N6O3
分子量:416.52
纯度:98%
存储:Store at -20°C

Background:

NCT-501 is a potent and selective theophylline-based inhibitor of aldehyde dehydrogenase 1A1 (ALDH1A1).Aldehyde dehydrogenases (ALDHs) metabolize reactive aldehydes and play important physiological and toxicological functions in metabolic disorders and cancers. ALDH1A1can be used as the marker of malignant prostate stem cells and predictor of prostate cancer patients' outcome. Over-expression of ALDH is associated with some types of cancers. Selective inhibitors targeted ALDH isozymes could preventspheroids formation in vitro and the size of xenograft tumors formed in vivo.

For more than 450 human kinases, NCT-501 treatment at 10 μM inhibited ≥55% activity of these kinases. NCT-501 reversibly inhibited ALDH1A1.The plasma exposure for intraperitoneal administration (ip) at 30 mg/kg showed better than the oral administration (p.o) at 30 mg/kg. The values of AUC 24h were 5670 h·ng/mL and 484 h·ng/mL along with 100% and 29% bioavailability, respectively. The t1/2 was shorter than 1h. The clearance level was 98 mL/min/kg. These results together indicated that NCT-501 was well absorbed and distributed but rapidly metabolized or excreted. In vitro stability of NCT-501in CD1 mouse plasma was more than 60 min.

Reference:
[1].Yang S M, Yasgar A, Miller B, et al.? Discovery of NCT-501, a Potent and Selective Theophylline-Based Inhibitor of Aldehyde Dehydrogenase 1A1 (ALDH1A1)[J]. Journal of medicinal chemistry, 2015, 58(15): 5967-5978.