AV-951 (Tivozanib) is a potent VEGFR-1, 2 and 3, c-Kit and PDGFR inhibitor with IC50 of 0.21, 0.16, 0.24, 1.63 and 1.72 nM respectively.AV-951 (Tivozanib) blocks the proliferation and migration of endothelial cells in vitro, and suppresses angiogenesis and growth of human tumor xenografts in vivo.
Cell Experiment | |
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Cell lines | HUVECs cells line |
Preparation method | Endothelial cell proliferation. HUVECs were seeded in M-199 (Invitrogen, Carlsbad, CA) containing 5% FBS in collagen-coated 96-well plates (BD Biosciences, Bedford, MA) at a density of 4,000 cells/200 μL/well. After 24 hours, KRN951 was added followed by 20 ng/mL VEGF or 10 ng/mL bFGF, and the cells were cultured for 72 hours. [3H]thymidine (1 μCi/mL) was added and the cells were cultured for a further 12 hours. Cells were then harvested and their radioactivity was measured with a Liquid Scintillation Counter (Wallac 1205 Beta Plate; Perkin-Elmer Life Sciences, Boston, MA). |
Concentrations | 0~1000nM |
Incubation time | 72h |
Animal Experiment | |
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Animal models | human tumor xenografts in athymic rats |
Formulation | 0.5% methyl cellulose in distilled water |
Dosages | 0.2 or 1 mg/kg for 14 days |
Administration | oral gavage |
Molecular Weight | 454.86 |
Formula | C22H19ClN4O5 |
CAS Number | 475108-18-0 |
Solubility (25°C) | DMSO 18 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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