Preclinical anticancer activity of the potent, oral Src inhibitor AZD0530
| العنوان: | Preclinical anticancer activity of the potent, oral Src inhibitor AZD0530 |
|---|---|
| المؤلفون: | Robin D. Whittaker, Geoffrey A. Holdgate, Vivien Jacobs, M. Fennell, Laurent Francois Andre Hennequin, Judith A. Hargreaves, Brigitte Boyer, Alun Bermingham, Tim P. Green, Jon Curwen, Walter H.J. Ward, Allen Jack Mcqueen, Paul Elvin, Robert W. Wilkinson, Gerard Costello, Patrick Ple, Neil O. Carragher, D. Mark Hickinson, Barry R. Davies, Armelle Logie |
| المصدر: | Green, T P, Fennell, M, Whittaker, R, Curwen, J, Jacobs, V, Allen, J, Logie, A, Hargreaves, J, Hickinson, D M, Wilkinson, R W, Elvin, P, Boyer, B, Carragher, N, Plé, P A, Bermingham, A, Holdgate, G A, Ward, W H J, Hennequin, L F, Davies, B R & Costello, G F 2009, ' Preclinical anticancer activity of the potent, oral Src inhibitor AZD0530 ', Molecular Oncology, vol. 3, no. 3, pp. 248-261 . https://doi.org/10.1016/j.molonc.2009.01.002Test |
| بيانات النشر: | John Wiley and Sons Inc., 2009. |
| سنة النشر: | 2009 |
| مصطلحات موضوعية: | Cancer Research, Transplantation, Heterologous, Administration, Oral, Mice, Nude, Antineoplastic Agents, Pharmacology, Metastasis, Mice, Rats, Nude, Clinical Trials, Phase II as Topic, In vivo, Cell Movement, Cell Line, Tumor, Genetics, medicine, Animals, Humans, Neoplasm Invasiveness, Benzodioxoles, Phosphorylation, Protein Kinase Inhibitors, Paxillin, Cell Proliferation, biology, Cell migration, General Medicine, medicine.disease, Xenograft Model Antitumor Assays, In vitro, Neoplasm Proteins, Rats, Transplantation, src-Family Kinases, Oncology, Urinary Bladder Neoplasms, Tumor progression, Focal Adhesion Kinase 1, Papers, biology.protein, NIH 3T3 Cells, Quinazolines, Molecular Medicine, Neoplasm Transplantation, Proto-oncogene tyrosine-protein kinase Src |
| الوصف: | 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 –> 10 μM). 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. |
| وصف الملف: | application/pdf |
| اللغة: | English |
| الوصول الحر: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::39828f060c31cb669d9f786b77db7400Test https://europepmc.org/articles/PMC5527863Test/ |
| حقوق: | OPEN |
| رقم الانضمام: | edsair.doi.dedup.....39828f060c31cb669d9f786b77db7400 |
| قاعدة البيانات: | OpenAIRE |
| الوصف غير متاح. |