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.2009.01.002
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.