Preclinical anticancer activity of the potent, oral Src inhibitor AZD0530.

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.

DOI: 10.1016/j.molonc.2009.01.002

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@article{Green2009PreclinicalAA, title={Preclinical anticancer activity of the potent, oral Src inhibitor AZD0530.}, author={Tim P. Green and Mike Fennell and Robin D Whittaker and Jon O. Curwen and Vivien N. Jacobs and Jack Allen and Armelle Logi{\'e} and Judith Hargreaves and D Mark Hickinson and Robert W. Wilkinson and Paul Elvin and Brigitte Boyer and Neil Oliver Carragher and Patrick A Pl{\'e} and Alun Bermingham and Geoffrey A Holdgate and Walter H. J. Ward and Laurent F A Hennequin and Barry R. Davies and Gerard F Costello}, journal={Molecular oncology}, year={2009}, volume={3 3}, pages={248-61} }