Src/Abl inhibitor,potent and selective
CAS：379231-04-6
分子式：C27H32ClN5O5
分子量：542.03
纯度：98%
存储：Store at -20°C

Background:

Saracatinib (AZD0530) is a novel, potent Src family kinase (SFK)/Abl dual-kinase inhibitor with IC50 value of 2.7 nM [1].

Saracatinib has been reported to inhibit Src activation in DU145 and PC3 cell lines (prostate cancer cell lines). Both of c-Myc and cyclin D1 expression are decreased by Saracatinib. Saracatinib can inhibit the ERK1/2 and GSK3b phosphorylation as well as decrease β-catenin level in cells. Saracatinib inhibits the prostate tumor cell growth by inducing cycle arrest at G1/S phase. Saracatinib dose-dependently blocks cell migration in DU145 and PC3 cell lines [1].

In DU145 implanted orthotopic SCID mice model, treatment with Saracatinib has been demonstrated to down-regulate the Src expression as well as suppress the tumor size [1].

参考文献:
[1] Chang YM1,?Bai L,?Liu S,?Yang JC,?Kung HJ,?Evans CP. Src family kinase oncogenic potential and pathways in prostate cancer as revealed by AZD0530. Oncogene.?2008 Oct 23;27(49):6365-75.