| Identification | Back Directory | [Name]
2H-Indol-2-one, 1,3-dihydro-5-methoxy-3-[[3-[(1E)-2-[6-(4-methyl-1-piperazinyl)-3-pyridinyl]ethenyl]-1H-indazol-6-yl]methylene]-, (3E)- | [CAS]
1169211-37-3 | [Synonyms]
2H-Indol-2-one, 1,3-dihydro-5-methoxy-3-[[3-[(1E)-2-[6-(4-methyl-1-piperazinyl)-3-pyridinyl]ethenyl]-1H-indazol-6-yl]methylene]-, (3E)- | [Molecular Formula]
C29H28N6O2 | [MOL File]
1169211-37-3.mol | [Molecular Weight]
492.57 |
| Hazard Information | Back Directory | [Description]
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. | [Uses]
CFI-400437 is an indolinone-derived, ATP-competitive kinase inhibitor with high selectivity for PLK4 (IC50 of 0.6 nM)[1]. | [in vivo]
CFI-400437 (25 mg/kg, ip, once daily for 21 d) exhibits antitumor activity against MDA-MB-468 breast cancer mouse xenograft model[1].
| [References]
[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 |
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