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- Title
Preclinical anticancer activity of the potent, oral Src inhibitor AZD0530
- Authors
Green, Tim P.; Fennell, Mike; Whittaker, Robin; Curwen, Jon; Jacobs, Vivien; Allen, Jack; Logie, Armelle; Hargreaves, Judith; Hickinson, D. Mark; Wilkinson, Robert W.; Elvin, Paul; Boyer, Brigitte; Carragher, Neil; Plé, Patrick A.; Bermingham, Alun; Holdgate, Geoffrey A.; Ward, Walter H.J.; Hennequin, Laurent F.; Davies, Barry R.; Costello, Gerard F.
- Abstract
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 (IC50 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.
- Subjects
ANTINEOPLASTIC agents; ENZYME inhibitors; ORAL drug administration; BLADDER cancer; LABORATORY mice; METASTASIS; CELL lines; TUMOR growth
- Publication
Molecular Oncology, 2009, Vol 3, Issue 3, p248
- ISSN
1574-7891
- Publication type
Article
- DOI
10.1016/j.molonc.2009.01.002