1169211-37-3

CFI-400437 is a potent and selective inhibitor of polo-like kinase 4 (PLK4). The family of Polo-like kinases is important in the regulation of mitotic progression; this work keys on one member, namely Polo-like kinase 4 (PLK4). PLK4 has been identified as a candidate anticancer target which prompted a search for potent and selective inhibitors of PLK4.

CFI-400437 is an indolinone-derived, ATP-competitive kinase inhibitor with high selectivity for PLK4 (IC50 of 0.6 nM)[1].

[1] Radoslaw Laufer, et al. The discovery of PLK4 inhibitors: (E)-3-((1H-Indazol-6-yl)methylene)indolin-2-ones as novel antiproliferative agents. J Med Chem. 2013 Aug 8;56(15):6069-87. DOI:10.1021/jm400380m
[2] Amreena Suri, et al. Evaluation of Protein Kinase Inhibitors with PLK4 Cross-Over Potential in a Pre-Clinical Model of Cancer. Int J Mol Sci. 2019 Apr 29;20(9):2112. DOI:10.3390/ijms20092112