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Vatalanib is an oral anti-angiogenesis agent that inhibits vascular endothelial growth factor receptor tyrosine kinases, which in patients showed auto induction of metabolism and variability in pharmacokinetic (PK) disposition. At higher concentrations, other tyrosine kinases are also inhibited, including PDGFR-β (IC₅₀ = 580 nM), c-KIT (IC₅₀ = 730 nM), FLT-4 (IC₅₀ = 660 nM) and c-FMS (IC₅₀ = 1.4 µM). On the other hand, vatalanib is not active against the EGFR, c-SRC, v-ABL, and protein kinase Cα (IC₅₀ > 10 µM). Vatalanib was well tolerated as a second-line therapy and resulted in favorable 6-month survival rate in patients with metastatic pancreatic cancer, compared with historic controls. The inhibitor Vatalanib is possibly an additional option in the treatment of leiomyosarcomas.
| Cell Experiment | |
|---|---|
| Cell lines | HUVECs |
| Preparation method | Endothelial Cell Proliferation Assays. As a test of the ability of PTK787/ZK 222584 to inhibit a functional response to VEGF, an endothelial cell proliferation assay, based on BrdUrd incorporation was used (Biotrak Cell Proliferation System V.2, Amersham, England). Subconfluent HUVECs were seeded at a density of 5 3 103 cells/well into 96-well plates coated with 1.5% gelatin and then incubated at 37°C and 5% CO2 in growth medium. After 24 h, growth medium was replaced by basal medium containing 1.5% FCS and a constant concentration of VEGF (50 ng/ml), bFGF (0.5 ng/ml), or FCS (5%), in the presence or absence of PTK787/ZK 222584. As a control, wells without growth factor were also included. After 24 h of incubation, BrdUrd labeling solution was added, and cells incubated an additional 24 h before fixation, blocking, and addition of peroxidase-labeled anti-BrdUrd antibody. Bound antibody was then detected using 3,395,59-tetramethylbenzidine substrate, which results in a colored reaction product that is quantified spectrophotometrically at 450 nm. |
| Concentrations | 0~1 μM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | Nude Mouse Human Tumor Xenograft Model |
| Formulation | distilled water |
| Dosages | 25 to 100 mg/kg once or twice dail |
| Administration | p.o. |
| Molecular Weight | 346.81 |
| Formula | C20H15ClN4 |
| CAS Number | 212141-54-3 |
| Solubility (25°C) | DMSO 25 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. |
| Tivozanib (AV-951)
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. |
| 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. |
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