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| Product Name: | Ki8751 | | Synonyms: | Ki8751 hydrate;Ki8751, >=98%;KI8751;KI 8751;KI-8751;VEGFR2 Kinase Inhibitor VI, Ki8751;Ki8751;1-(2,4-Difluoro-phenyl)-3-[4-(6,7-dimethoxy-quinolin-4-yloxy)-2-fluoro-phenyl]-urea hydrate;N-(2,4-Difluorophenyl)-N'-[4-[(6,7-dimethoxy-4-quinolinyl)oxy]-2-fluorophenyl]urea;1-(2,4-difluorophenyl)-3-(4-(6,7-diMethoxyquinolin-4-yloxy)-2-fluorophenyl)urea | | CAS: | 228559-41-9 | | MF: | C24H18F3N3O4 | | MW: | 469.41 | | EINECS: | | | Product Categories: | Inhibitors | | Mol File: | 228559-41-9.mol |  |
| | Ki8751 Chemical Properties |
| 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. |
| Hazard Codes | Xn | | Risk Statements | 22-38 | | Safety Statements | 37 |
| | Ki8751 Usage And Synthesis |
| 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 | | Uses | 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. | | Uses | 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. | | 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 |
| | Ki8751 Preparation Products And Raw materials |
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