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Nintedanib (BIBF1120)

Cat. No. M1673
Nintedanib (BIBF1120) Structure
Synonym:

Nintedanib

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL USD 45  USD45 In stock
5mg USD 30  USD30 In stock
10mg USD 40  USD40 In stock
50mg USD 75  USD75 In stock
100mg USD 100  USD100 In stock
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Quality Control & Documentation
Biological Activity

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

Customer Product Validations & Biological Datas
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
Protocol (for reference only)
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
Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Xiao et al. Eur J Clin Pharmacol. Chemotherapy plus multitargeted antiangiogenic tyrosine kinase inhibitors or chemotherapy alone in advanced NSCLC: a meta-analysis of randomized controlled trials.

[2] Günther et al. Eur Respir Rev. Unravelling the progressive pathophysiology of idiopathic pulmonary fibrosis.

[3] Doebele et al. Ann Oncol. A phase I, open-label dose-escalation study of continuous treatment with BIBF 1120 in combination with paclitaxel and carboplatin as first-line treatment in patients with advanced non-small-cell lung cancer.

[4] Gori et al. Ther Clin Risk Manag. New antiangiogenics in non-small cell lung cancer treatment: Vargatef™ (BIBF 1120) and beyond.

[5] Bousquet et al. Br J Cancer. Phase I study of BIBF 1120 with docetaxel and prednisone in metastatic chemo-naive hormone-refractory prostate cancer patients.

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