Nintedanib (BIBF1120) is an indolinone derivative potently blocking VEGF receptor (VEGFR), PDGFR and FGFR kinase activity in enzymatic assays (IC50, 20–100 nmol/L). 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.
Another CAS# 656247-17-5
Cell Experiment | |
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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 | |
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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 ≥ 20 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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