CFI-400437

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

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> Polo-like Kinase (PLK)

CFI-400437 is a potent inhibitor of MCF-7, MDA-MB-468 and MDA-MB231 cell growth[1]. CFI-400437 inhibits Aurora A, Aurora B, KDR and FLT-3 with IC50s of 0.37, 0.21, 0.48, and 0.18 µM, respectively, i.e. two orders of magnitude higher than its IC50 of 0.6 nM against PLK4[1]. CFI-400437 inhibits both AURKB and AURKC at concentrations <15 nM[2].

CFI-400437 (25 mg/kg, ip, once daily for 21 d) exhibits antitumor activity against MDA-MB-468 breast cancer mouse xenograft model[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.

[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.