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 > CB-839
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:
 
CB-839
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。
CB-839图片
CAS NO:1439399-58-2
规格:98%
分子量:571.57
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
glutaminase inhibitor
CAS:1439399-58-2
分子式:C26H24F3N7O3S
分子量:571.57
纯度:98%
存储:Store at -20°C

Background:

Telaglenastat (CB-839) is a first-in-class, reversible and orally bioavailable glutaminase 1 (GLS1) inhibitor. Telaglenastat (CB-839) selectively inhibits GLS1 splice variants KGA (kidney-type glutaminase) and GAC (glutaminase C) compared to GLS2. The IC50s are 23 and 28 nM for endogenous glutaminase in mouse kidney and brain, respectively. Antitumor activity[1].


Telaglenastat (CB-839) (0.1-1000 nM; 72 hours) has antiproliferative activity in HCC1806 and MDA-MB-231 cells with IC50s of 49 nM and 26 nM, respectively[1].Telaglenastat (CB-839) (1 μM; 72 hours) activates caspase 3/7 and induces apoptosis in MDA-MB-231 and HCC1806 cells[1].


Telaglenastat (CB-839) (200 mg/kg; p.o.; twice daily for 28 days) has antitumor activity in xenograft models of TNBC[1].


参考文献:
[1]. Gross MI, et al. Antitumor activity of the glutaminase inhibitor CB-839 in triple-negative breast cancer. Mol Cancer Ther. 2014 Apr;13(4):890-901.
[2]. Biancur DE, et al. Compensatory metabolic networks in pancreatic cancers upon perturbation of glutaminemetabolism. Nat Commun. 2017 Jul 3;8:15965.