Name | Ki8751 |
Synonyms | Ki8751 KI8751 KI 8751 KI-8751 Ki8751 hydrate VEGFR2 Kinase Inhibitor VI, Ki8751 1-(2,4-difluorophenyl)-3-(4-(6,7-diMethoxyquinolin-4-yloxy)-2-fluorophenyl)urea N-(2,4-Difluorophenyl)-N'-[4-[(6,7-dimethoxy-4-quinolinyl)oxy]-2-fluorophenyl]urea 1-(2,4-Difluoro-phenyl)-3-[4-(6,7-dimethoxy-quinolin-4-yloxy)-2-fluoro-phenyl]-urea hydrate |
CAS | 228559-41-9 |
Molecular Formula | C24H18F3N3O4 |
Molar Mass | 469.41 |
Density | 1.429 |
Melting Point | 239℃ |
Solubility | Soluble in DMSO (15 mg/ml) |
Appearance | Off-white solid |
Color | White |
Storage Condition | −20°C |
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. |
In vitro study | Ki8751 was potent and selective for VEGFR-2 inhibition with an IC50 of 0.9 nM. Ki8751 also inhibited PDGFRα by c-Kit, and FGFR-2, with higher IC50 values (40 nM-170 nM). In addition to the above kinases, Ki8751 did not inhibit other kinases, including HGFR, EGFR, and InsulinR, even at a concentration of 10 μm. 1 nM-100 nM Ki8751 acts on human umbilical vein endothelial cells (HUVECs), and Ki8751(1 nM-100 nM) effectively reduces VEGF-stimulated cell proliferation and vascular permeability. 10 nM Ki8751 acts on metastatic colorectal cancer (CRC) cells MIP, RKO, SW620, and SW480, but not HCT116, promoting cellular senescence. |
In vivo study | Ki8751 inhibited tumor growth at a dose of 20 mg/kg in mice bearing human xenografts of GL07, St-4, LC6, DLD-1, and a375. Ki8751 at the dose of 5 mg/kg in nude mice with LC-6 of the transplanted tumor completely inhibited tumor growth, and did not affect the body weight of the mice. |
Hazard Symbols | Xn - Harmful |
Risk Codes | R22 - Harmful if swallowed R38 - Irritating to the skin |
Safety Description | 37 - Wear suitable gloves. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.13 ml | 10.652 ml | 21.303 ml |
5 mM | 0.426 ml | 2.13 ml | 4.261 ml |
10 mM | 0.213 ml | 1.065 ml | 2.13 ml |
5 mM | 0.043 ml | 0.213 ml | 0.426 ml |