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Tivozanib (AV-951) 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. Tivozanib (AV-951) blocks the proliferation and migration of endothelial cells in vitro, and suppresses angiogenesis and growth of human tumor xenografts in vivo.
| Cell Experiment | |
|---|---|
| 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 | |
|---|---|
| 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 |
| Related VEGFR/PDGFR Products |
|---|
| ABT-869
ABT-869 (Linifanib) is an ATP-competitive, multi-targeted RTK inhibitor that is completely effective against all members of VEGFR and PDGFR. |
| Axitinib
Axitinib (AG013736) inhibits multiple targets including VEGFR, PDGFR and cKit. |
| Regorafenib
Regorafenib (BAY 73-4506) is a novel oral multikinase inhibitor of c-KIT, VEGFR2, B-Raf with IC50s of 17, 40 and 69 nM respectively. |
| Nintedanib
Nintedanib (BIBF1120) is a novel, potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively. |
| Brivanib alaninate
Brivanib alaninate (BMS-582664) is a novel, orally available and selective receptor tyrosine kinase inhibitor of VEGF-R2 and FGF-R1 and -2. |
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