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PHA-739358, a potent inhibitor of Aurora kinases with a selective target inhibition profile relevant to cancer

1 Dec 2007

Abstract excerpt

PHA-739358 is a small-molecule 3-aminopyrazole derivative with strong activity against Aurora kinases and cross-reactivities with some receptor tyrosine kinases relevant for cancer. PHA-739358 inhibits all Aurora kinase family members and shows a dominant Aurora B kinase inhibition-related cellular phenotype and mechanism of action in cells in vitro and in vivo. p53 status-dependent endoreduplication is observed...

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PMID: 18089710
DOI: 10.1158/1535-7163.mct-07-0444

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