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HomeProduct name listKi8751

Ki8751

Synonym(s):N-(2,4-Difluorophenyl)-N?-(4-(6,7-dimethoxy-4-quinolyloxy)-2-fluorophenyl)urea, Vascular Endothelial Growth Factor Receptor 2 Kinase Inhibitor VI, VEGFR Tyrosine Kinase Inhibitor XXIV;VEGFR2 Kinase Inhibitor VI, Ki8751 - CAS 228559-41-9 - Calbiochem

Ki8751 Structural

What is Ki8751?

Description

Ki8751 (228559-41-9) is a very potent (IC50 = 0.9 nM) inhibitor of vascular endothelial growth factor receptor 2 (VEGFR-2).1 It also inhibited PDGFRα (IC50 = 67 nM), c-Kit (IC50 = 40 nM), and FGFR2 (IC50 = 170 nM). Ki8751 completely suppressed HUVEC growth at 1 nM. Ki8751 completely inhibited tumor growth in LC-6 human tumor xenografts @ 5mg/kg. Ki8751 displayed anti-influenza A and B activity via disruption of virus entry in a PDGFR?/GM3-dependent manner.2

The Uses of Ki8751

Ki8751 is a potent and selective inhibitor of VEGFR2, PDGFRα and c-Kit with IC50 of 0.9 nM, 67 nM and 40 nM, respectively.

The Uses of Ki8751

KI 8751 is a potent and selective inhibitor of VEGFR-2-tyrosine kinase which inhibits proliferation of human umbilical vein endothelial cells and inhibits tumor growth.

What are the applications of Application

KI 8751 is a cell-permeable Flk-1 (VEGFR-2) and c-Kit inhibitor

Definition

ChEBI: 1-(2,4-difluorophenyl)-3-[4-[(6,7-dimethoxy-4-quinolinyl)oxy]-2-fluorophenyl]urea is an aromatic ether.

General Description

A cell-permeable quinolyloxyphenyl-urea compound that acts as a VEGFR-2-selective inhibitior in both cell-based (IC50 = 0.9 nM in VEGF-induced receptor phosphorylation) and cell-free (IC50 = 4.0 nM in kinase reactions) assays. It inhibits c-Kit, PDGFRα, and FGFR-2 only at much higher concentrations (IC50 = 40, 67, and 170 nM, respectively, in cell-based assays), while exhibiting no effect against eight other commonly studied receptor and non-receptor kinases even at concentrations as high as 10 μM. Effectively blocks VEGF-dependent, but not VEGF-independent, cell proliferation in vitro and tumor growth in mice and rats (5 to 20 mg/kg, daily p.o.) in vivo.

Biological Activity

Potent, selective inhibitor of VEGFR-2 tyrosine kinase (IC 50 = 0.9 nM). Displays some inhibitory activity towards c-Kit, PDGFR α and FGFR-2 (IC 50 values range from 40 to 170 nM) but is highly selective over other receptor tyrosine kinases (IC 50 > 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.

storage

Store at +4°C

References

Kubo et al. (2005), 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 1359 Vrijens et al. (2019), Influenza virus entry via the GM3 ganglioside-mediated platelet-derived growth factor receptor b signaling pathway; J. Gen. Virol. 100 583

Properties of Ki8751

Melting point: 239℃
Density  1.429
storage temp.  −20°C
solubility  Soluble in DMSO (15 mg/ml)
form  Off-white solid
color  White
Stability: Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.

Safety information for Ki8751

Computed Descriptors for Ki8751

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