CFI-400945 is an orally available, selective inhibitor of polo-like kinase 4 (PLK4; IC₅₀ = 2.8 nM), a unique kinase that regulates centriole duplication during the cell cycle.¹ It does not inhibit other members of the PLK family (IC₅₀s > 50 µM for PLK1, PLK2, and PLK3).¹ CFI-400945 has been shown to dysregulate centriole duplication, disrupt mitosis, and induce apoptosis in various PLK4-overexpressing breast cancer cells and to reduce tumor growth in mice bearing MDA-MB-468 breast tumor xenografts.¹

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1.Mason, J.M.,Lin, D.C.,Wei, X., et al. Functional characterization of CFI-400945, a polo-like kinase 4 inhibitor, as a potential anticancer agent. Cancer Cell 26(2), 163-176 (2014).