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Ki8751 (CAS 228559-41-9) LS-H149

VEGFR2 inhibitor
LS-H149-5 / 5 mg / $195
LS-H149-10 / 10 mg / $225
LS-H149-25 / 25 mg / $295
LS-H149-50 / 50 mg / $415
USA Shipment Only
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Description: Vascular endothelial growth factor receptor 2 (VEGFR2, also known as KDR and FLK1) is a receptor tyrosine kinase that regulates angiogenesis, vascular development, and embryonic hematopoiesis in response to VEGF isoforms A, C, and D. Ki8751 is a potent, orally available inhibitor of the kinase activity of VEGFR2 (IC50 = 0.9 nM). It less potently inhibits c-Kit, PDGRF alpha, and FGFR2 (IC50s = 40-170 nM) and has no significant effect against several other receptor tyrosine kinases. Ki8751 suppresses the growth of VEGF-stimulated human µMbilical vein endothelial cells at nanomolar concentrations. It shows significant anti-tumor activity against assorted human tumor xenografts in nude mice. Ki8751 also induces cellular senescence in colorectal cancer cells. H149_ChemicalStructureImage.png
biochemical, chemical, inhibitor
A crystalline solid
Shipped Ambient, store at -20°C, ≥ 2 years shelf life.
This product is for research use only. Not for administration to humans, or for human or veterinary diagnostic or therapeutic use.
Data Sheet DataSheet    SDS SDS
Related Products: KDR / VEGFR2 / FLK1 related products

Usage Information

Ki8751 is supplied as a crystalline solid. A stock solution may be made by dissolving the Ki8751 in the solvent of choice. Ki8751 is soluble in organic solvents such as DMSO and dimethyl formamide (DMF), which should be purged with an inert gas. The solubility of Ki8751 in these solvents is approximately 20 and 25 mg/ml, respectively. Ki8751 is sparingly soluble in aqueous buffers. For maximum solubility in aqueous buffers, Ki8751 should first be dissolved in DMF and then diluted with the aqueous buffer of choice. Ki8751 has a solubility of approximately 0.25 mg/ml in a 1:3 solution of DMF:PBS (pH 7.2) using this method. We do not recommend storing the aqueous solution for more than one day.

  1. Kubo, K., Shimizu, T., Ohyama, S., et al. Novel potent orally active selective VEGFR-2 tyrosine kinase inhibitors: Synthesis, structure-activity relationships, and antitumor activities of N-phenyl-N’-{4-(4- quinolyloxy)phenyl}ureas. J. Med. Chem. 48(5), 1359-1366 (2005).
  2. Hasan, M.R., Ho, S.H.Y., Owen, D.A., et al. Inhibition of VEGF induces cellular senescence in colorectal cancer cells. Int. J. Cancer 129(9), 2115-2123 (2011).


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