Sell PF-03814735

Description

PF PF********5 is a novel, potent, orally bioavailable, reversible small-molecule Aurora kinase inhibitor with IC*0 of 0.8, 5, *0 and *2 nM for Aurora 1, Aurora 2, Flt 1 and FAk, respectively. Aurora kinases are serine- threonine kinases that play essential roles in mitotic checkpoint control during mitosis. PF********5 possesses potential antineoplastic activity. Aurora kinase inhibitor PF********5 binds to and blocks Aurora kinases A and B, which may result in the prevention of cellular division and proliferation in tumor cells that overexpress these kinases. In intact cells, the preventive activity of PF********5 on the Aurora1 and Aurora2 kinases attenuates levels of phospho-Aurora1, phosphohistone H3, and phospho-Aurora2