Catalog Number: 2542
Chemical Name: N-(2,4-Difluorophenyl)-N'-[4-[(6,7-dimethoxy-4-quinolinyl)oxy]-2-fluorophenyl]urea
Biological Activity
Potent, selective inhibitor of VEGFR-2 tyrosine kinase (IC50 = 0.9 nM). Displays some inhibitory activity towards c-Kit, PDGFRα and FGFR-2 (IC50 values range from 40 to 170 nM) but is highly selective over other receptor tyrosine kinases (IC50 > 10000 nM for FGFR-2, EGFR and HGFR). Inhibits VEGF-stimulated proliferation of human umbilical vein endothelial cells (HUVEC) and inhibits tumor growth in vivo; antiangiogenic.
Technical Data
  • M.Wt:
    469.41
  • Formula:
    C24H18F3N3O4
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
    >97%
  • Storage:
    Store at +4°C
  • CAS No:
    228559-41-9
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Novel potent orally active selective VEGFR-2 tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumour activities of N-phenyl-N'-{4-(4-quinolyloxy)phenyl}ureas.
    Kubo et al.
    J.Med.Chem., 2005;48:1359
Citations:

The citations listed below are publications that use Tocris products. Selected citations for Ki 8751 include:

1 Citations: Showing 1 - 1

  1. Investigation of a novel molecular descriptor for the lead optimization of 4-aminoquinazolines as vascular endothelial growth factor receptor-2 inhibitors: application for quantitative structure-activity relationship analysis in lead optimization.
    Authors: Kawakami Et al.
    J Neurosci 2011;21:1371

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