您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > ABC294640
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:
 
ABC294640
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。
ABC294640图片
CAS NO:915385-81-8
规格:98%
分子量:380.91
包装与价格:
包装价格(元)
5mg电议
25mg电议
100mg电议

产品介绍
Sphingosine kinase 2 inhibitor,selective and competitive
CAS:915385-81-8
分子式:C23H25ClN2O
分子量:380.91
纯度:98%
存储:Store at -20°C

Background:

ABC294640 is a selective and competitive inhibitor of sphingosine kinase 2 (SK2) with IC50 value of 60μM [1].


ABC294640 is a competitive inhibitor of SK2. It shows IC50 value of about 60μM against recombinant human SK2. In the kinetic assay, ABC294640 competes with sphingosine and exerts a Ki value of 9.8μM. Because of its targeting of the sphingosine binding site of SK2, ABC294640 shows no inhibition activity against other 20 kinases. In MDA-MB-231 cells, ABC294640 prevents S1P production with IC50 value of 26μM. Moreover, ABC294640 has anti-proliferation and anti-migration efficacies in tumor cells. It suppresses cell proliferation of a variety of tumor cell lines such as 1025LU, A-498, Caco-2 and HT-29. The IC50 values are ranged from 6μM to 48μM. Furthermore, administration of ABC294640 inhibits tumor growth in the immunocompetent BALB/c mice bearing mammary adenocarcimona xenografts. Besides that, ABC294640 is also found to have greater anti-proliferation effects in ER-positive than ER-negative breast cancer cells. The effect of E2 signaling caused by ABC294640 is expected to be a therapeutic in endocrine-related diseases [1, 2].


参考文献:
[1] French K J, Zhuang Y, Maines L W, et al. Pharmacology and antitumor activity of ABC294640, a selective inhibitor of sphingosine kinase-2. Journal of Pharmacology and Experimental Therapeutics, 2010, 333(1): 129-139.
[2] Antoon J W, White M D, Meacham W D, et al. Antiestrogenic effects of the novel sphingosine kinase-2 inhibitor ABC294640. Endocrinology, 2010, 151(11): 5124-5135.