Saracatinib, Free Base (AZD-0530, CAS 379231-04-6), >99%

LC Laboratories' Product Number S-8906 - Saracatinib, Free Base (AZD-0530, CAS 379231-04-6), >99% - for research use only. Saracatinib an orally available Src kinase inhibitor. Saracatinib inhibits c-Src and Abl enzymes at low nanomolar concentrations. Saracatinib blocked the tumor growth of a c-Src-transfected 3T3-fibroblast xenograft in vivo and increased significantly the survival of animals in a highly aggressive model of human pancreatic cancer. Saracatinib blocked the proliferation of various cell lines tested (IC50 = 0.2 - >10 µM) and inhibited tumor growth in 4/10 xenograft models tested. Saracatinib had significant antimigratory and anti-invasive effects in vitro, and inhibited metastasis of bladder cancer in vivo. Saracatinib blocked phosphorylation of Src substrates paxillin and FAK in both growth-inhibition-resistant and -sensitive xenografts. Saracatinib blocked the growth of, and induced apoptosis in, chronic myeloid leukaemia (CML) and Ph+ acute lymphoblastic leukaemia (ALL) cells, but showed only slight effects on Ph- ALL cells. Saracatinib overcame the resistance to imatinib due to the mutation Y253F in p185Bcr-Abl. Combination treatment of saracatinib and imatinib showed an additive inhibitory effect on the proliferation of CML BV173 cells but not on Ph+ ALL SupB15 cells. Saracatinib inhibited the anchorage-dependent growth of MCF-7 with IC50 of 0.47 µM, which was increased 4-fold in the presence of estrogen. In contrast, saracatinib inhibited the growth of cells stably expressing the mutant ERα with an elevated IC50 that was only increased 1.4-fold by estrogen stimulation. The results indicated that c-Src inhibition is blocked by estrogen signaling. Saracatinib inhibited the proliferation of DU145 and PC3 prostate cancer cells, apparently by reducing binding of beta-catenin to the promoters of G1 phase cell cycle regulators cyclin D1 and c-Myc. Saracatinib also decreased orthotopic DU145 xenograft growth by 45% in mice. Saracatinib treatment is feasible and tolerable in previously treated patients suffering from advanced castration-resistant prostate cancer, but it had little clinical efficacy as monotherapy.

• Supplier: LC Laboratories
• Product #: S-8906
• Sku #: S-8906_2g