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PHA-767491 is a potent inhibitor of Cdc7 kinase with an IC50 value of 10 nM in the presence of 1.5 µM ATP.1 At 10 µM, PHA-767491 induces apoptotic cell death in multiple cancer cell types.1 PHA-767491 also inhibits Cdk9, a kinase involved in the phosphorylation of RNA polymerase II and in transcriptional regulation of gene expression, with an IC50 value of 34 nM.2
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1. A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity. Nat. Chem. Biol. 4(6), 357-365 (2008).
2. First Cdc7 kinase inhibitors: Pyrrolopyridinones as potent and orally active antitumor agents. 2. lead discovery. J. Med. Chem. 52(2), 293-307 (2009).