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Biological Activity:
A highly potent and selective polo-like kinase (PLK) 1 inhibitor (enzyme IC50 = 0.87 nM, EC50 = 11-37 nM on a panel of cancer cell lines), which exhibited significant anti-proliferative in multiple cancer models, including a model of taxane-resistant colorectal cancer.
A high volume of distribution, indicating good tissue penetration, and a long terminal half-life have emerged as distinct features of BI 6727, which may have a favorable effect on antitumor efficacy in vivo.
References: online
D Rudolph et al. BI 6727, a Polo-like kinase inhibitor with improved pharmacokinetic profile and broad antitumor activity. Clin. Cancer Res. 2009, 15(9), 3094-3102. [online]
P Schöffski. Polo-like kinase (PLK) inhibitors in preclinical and early clinical development in oncology. Oncologist. 2009, 14(6), 559-570. [Review]
Chemical Name: N-[trans-4-(4-Cyclopropylmethyl-piperazin-1-yl)-cyclohexyl]-4-((R)-7-ethyl-8-isopropyl-5-methyl-6-oxo-5,6,7,8-tetrahydro-pteridin-2-ylamino)-3-methoxy-benzamide
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