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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.
Nintedanib (BIBF1120) inhibits mitogen-activated protein kinase and Akt signaling pathways in three cell types contributing to angiogenesis, endothelial cells, pericytes, and smooth muscle cells, resulting in inhibition of cell proliferation (EC50, 10–80 nmol/L) and apoptosis.
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Source | Oncotarget (2015). Figure 5. BIBF1120 |
| Method | Western blots | |
| Cell Lines | SKOV3 cells | |
| Concentrations | 5 μM | |
| Incubation Time | 24 h | |
| Results | We utilized a custom-made siRNA library for the six mesenchymal signature genes to test the differences in the nintedanib effects on E-cadherin induction |
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Source | Oncotarget (2015). Figure 4. BIBF1120 |
| Method | Western blots | |
| Cell Lines | SKOV3 cells | |
| Concentrations | 5 μM | |
| Incubation Time | 24 h | |
| Results | Furthermore, 5 μM nintedanib concomitantly up-regulated both E-cadherin protein and CDH1 transcript levels |
| Cell Experiment | |
|---|---|
| Cell lines | HUVEC, HSMEC, BRP, HUASMC, FaDu, Calu-6 and Hela cells line |
| Preparation method | Cell proliferation and apoptosis assays.[3H]Thymidine incorporation assay for proliferation analysis and apoptosis assay was performed as previously described. |
| Concentrations | 0~5µM |
| Incubation time | 72 h |
| Animal Experiment | |
|---|---|
| Animal models | Human FaDu (squamous cell carcinoma of the head and neck) xenografts growing in nude mice |
| Formulation | not mentioned |
| Dosages | 10, 50, 100 mg/kg |
| Administration | orally |
| Molecular Weight | 539.62 |
| Formula | C31H33N5O4 |
| CAS Number | 656247-17-5 |
| Solubility (25°C) | DMSO 6 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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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. |
| Axitinib
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| Regorafenib
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| 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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