All AbMole products are for research use only, cannot be used for human consumption.
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.
 |
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 |
 |
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 |
| Related VEGFR/PDGFR Products |
|---|
| Ramucirumab
Ramucirumab is a direct VEGFR2 antagonist, that binds with high affinity to the extracellular domain of VEGFR2 and block the binding of natural VEGFR ligands (VEGF-A, VEGF-C and VEGF-D). |
| 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. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2024 AbMole BioScience. All Rights Reserved.
