1169211-37-3

1169211-37-3 structure
1169211-37-3 structure
  • Name: CFI-400437
  • Chemical Name: CFI-400437
  • CAS Number: 1169211-37-3
  • Molecular Formula: C29H28N6O2
  • Molecular Weight: 492.57
  • Catalog: Signaling Pathways Cell Cycle/DNA Damage Polo-like Kinase (PLK)
  • Create Date: 2021-12-19 20:31:36
  • Modify Date: 2024-01-09 12:43:50
  • CFI-400437 is an indolinone-derived, ATP-competitive kinase inhibitor with high selectivity for PLK4 (IC50 of 0.6 nM)[1].

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

[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.

Molecular Formula C29H28N6O2
Molecular Weight 492.57