| Literature DB >> 19393585 |
Tim P Green1, Mike Fennell, Robin Whittaker, Jon Curwen, Vivien Jacobs, Jack Allen, Armelle Logie, Judith Hargreaves, D Mark Hickinson, Robert W Wilkinson, Paul Elvin, Brigitte Boyer, Neil Carragher, Patrick A Plé, Alun Bermingham, Geoffrey A Holdgate, Walter H J Ward, Laurent F Hennequin, Barry R Davies, Gerard F Costello.
Abstract
AZD0530, an orally available Src inhibitor, demonstrated potent antimigratory and anti-invasive effects in vitro, and inhibited metastasis in a murine model of bladder cancer. Antiproliferative activity of AZD0530 in vitro varied between cell lines (IC(50) 0.2 ->10μM). AZD0530 inhibited tumor growth in 4/10 xenograft models tested and dynamically inhibited in vivo phosphorylation of Src substrates paxillin and FAK in both growth-inhibition-resistant and -sensitive xenografts. The activity of AZD0530 in NBT-II bladder cancer cells in vitro was consistent with inhibition of cell migration and stabilization of cell-cell adhesion. These data suggest a dominant anti-invasive pharmacology for AZD0530 that may limit tumor progression in a range of cancers. AZD0530 is currently in Phase II clinical trials.Entities:
Mesh：
Substances：
Year: 2009 PMID： 19393585 PMCID： PMC5527863 DOI： 10.1016/j.molonc.2009.01.002
Source DB: PubMed Journal: Mol Oncol ISSN： 1574-7891 Impact factor: 6.603