[HTML][HTML] Preclinical anticancer activity of the potent, oral Src inhibitor AZD0530
TP Green, M Fennell, R Whittaker, J Curwen… - Molecular …, 2009 - Elsevier
TP Green, M Fennell, R Whittaker, J Curwen, V Jacobs, J Allen, A Logie, J Hargreaves…
Molecular oncology, 2009•ElsevierAZD0530, 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 …
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 …
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.
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