Unknown

Dataset Information

0

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.

SUBMITTER: Green TP 

PROVIDER: S-EPMC5527863 | biostudies-other | 2009 Jun

REPOSITORIES: biostudies-other

Similar Datasets

| S-EPMC2569026 | biostudies-literature
| S-EPMC6546470 | biostudies-literature
| S-EPMC4381587 | biostudies-literature
2012-07-19 | E-GEOD-38008 | biostudies-arrayexpress
2015-03-18 | GSE62460 | GEO
| S-EPMC2663092 | biostudies-literature
| S-EPMC4467398 | biostudies-literature
| S-EPMC4493896 | biostudies-other
2012-07-20 | GSE38008 | GEO
| S-EPMC6119657 | biostudies-literature