Ki 8751

Cat. No. 2542

Ki 8751 C24H18F3N3O4 [228559-41-9]

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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.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Kubo et al (2005) 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. J.Med.Chem. 48 1359. PMID: 15743179.

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Citations are publications that use Tocris products. Selected citations for Ki 8751 include:

Kawakami et al (2011) 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. J Neurosci 21 1371. PMID: 21306896.

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Keywords: Ki 8751, supplier, Potent, selective, VEGFR-2, inhibitors, inhibits, Vascular, Endothelial, Growth, Factors, Receptors, KDR, Flt, Receptor, Tyrosine, Kinases, RTKs, Ki8751, Tocris Bioscience, VEGFR Inhibitor products

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