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BI 6727 is a highly potent Polo-like kinase inhibitor with an IC50 of 0 .87 nM BI 6727 has an EC50 of 11-37 nM on a panel of cancer cell lines and selective dihydropteridinone with distinct properties. BI 6727 has a pharmacokinetic profile favoring sustained exposure of tumor tissues with a high volume of distribution and a long terminal half-life in mice. BI 6727 has physicochemical and pharmacokinetic properties that allow in vivo testing of i.v. as well as oral formulations, adding flexibility to dosing schedules. BI 6727 shows marked antitumor activity in multiple cancer models, including a model of taxane-resistant colorectal cancer. ^[1][2][3]

• BI 6727, A Polo-like Kinase Inhibitor with Improved Pharmacokinetic Profile and Broad Antitumor Activity Martin Steegmaier, Matthias Hoffmann, et al. Clin Cancer Res 2009;15:3094-3102
• Polo-Like Kinase (PLK) Inhibitors in Preclinical and Early Clinical Development in Oncology PATRICK SCHÖFFSKI The Oncologist 2009;14:559–570
• Small Molecule Kinase Inhibitor Screen Identifies Polo-Like Kinase 1 as a Target for Neuroblastoma Tumor-Initiating Cells Alessandro Datti, Mayumi Fujitani, et al. Cancer Res 2011;71:1385-1395

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