| 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 |