Ki 8751

Biological Activity

Ki 8751 is a 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

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Glucagon-like peptide-2 directly regulates hypothalamic neurons expressing neuropeptides linked to appetite control in vivo and in vitro.
   Dalvi PS, Belsham DD
   Endocrinology, 2012;153(5):2385-97.
2. 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

Product Datasheets