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BIBF1120

Cat. No. M1673
BIBF1120 Structure
Synonym:

Vargatef

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM/1mL In DMSO USD 70 In stock
10mg USD 60 In stock
50mg USD 180 In stock
100mg USD 350 In stock
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Quality Control
Biological Activity

BIBF 1120 is an indolinone derivative potently blocking VEGF receptor (VEGFR), PDGFR and FGFR kinase activity in enzymatic assays (IC50, 20–100 nmol/L). BIBF 1120 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.

Protocol
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 539.62
Formula C31H33N5O4
CAS Number 928326-83-4, 656247-17-5
Purity 99.46%
Solubility DMSO
Storage at -20°C
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
Rating
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
Rating
References

Chemotherapy plus multitargeted antiangiogenic tyrosine kinase inhibitors or chemotherapy alone in advanced NSCLC: a meta-analysis of randomized controlled trials.
Xiao et al. Eur J Clin Pharmacol. 2012 Jun 24. PMID: 22729611.

Unravelling the progressive pathophysiology of idiopathic pulmonary fibrosis.
Günther et al. Eur Respir Rev. 2012 Jun 1;21(124):152-60. PMID: 22654088.

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.
Doebele et al. Ann Oncol. 2012 Aug;23(8):2094-102. PMID: 22345119.

New antiangiogenics in non-small cell lung cancer treatment: Vargatef™ (BIBF 1120) and beyond.
Gori et al. Ther Clin Risk Manag. 2011;7:429-40. PMID: 22241943.

Phase I study of BIBF 1120 with docetaxel and prednisone in metastatic chemo-naive hormone-refractory prostate cancer patients.
Bousquet et al. Br J Cancer. 2011 Nov 22;105(11):1640-5. PMID: 22027711.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: BIBF1120, Vargatef supplier, VEGFR/PDGFR, inhibitors

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