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Nintedanib Ethanesulfonate Salt

Cat. No. M6197
Nintedanib Ethanesulfonate Salt Structure
Synonym:

BIBF 1120 esylate

Size Price Availability Quantity
10mg USD 95 In stock
50mg USD 255 In stock
100mg USD 400 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

In vitro: BIBF 1120 binds to the ATP-binding site in the cleft between the amino and carboxy terminal lobes of the kinase domain. BIBF 1120 inhibits proliferation of PDGF-BB stimulated BRPs with EC50 of 79 nM in cell assays. BIBF1120 (100 nM) blocks activation of MAPK after stimulation with 5% serum plus PDGF-BB. BIBF1120 prevents PDGF-BB stimulated proliferation with an EC50 of 69 nM in cultures of human vascular smooth muscle cells (HUASMC).

In vivo: BIBF1120 (25-100 mg/kg daily p.o.) is highly active in all tumor models, including human tumor xenografts growing in nude mice and a syngeneic rat tumor model. This is evident in the magnetic resonance imaging of tumor perfusion after 3 days, reducing vessel density and vessel integrity after 5 days, and profound growth inhibition. BIBF1120 is orally available and displays encouraging efficacy in in vivo tumor models while being well tolerated.

Protocol
Cell Experiment
Cell lines HUVEC, HUASMC, and BRP cell lines
Preparation method The cell lines HUVEC, HUASMC, and BRP are used for the assay. BIBF1120 is added to the cultures two hours before the addition of ligands. Cell lysates are generated. Western blotting is done using standard SDS-PAGE methods, loading 50 to 75 μg of protein per lane. Detection is facilitated by enhanced chemiluminescence. Total and phosphorylated mitogen-activated protein kinase (MAPK) is analyzed using monoclonal antibodies M3807 and M8159. Total Akt is detected using the corresponding polyclonal antibody and phosphorylated Akt (Ser473) is analyzed by using its monoclonal antibody. Monoclonal antibody is also used to detect cleaved caspase-3 while KDR (VEGFR2) protein is detected using a corresponding antibody.
Concentrations 50 nM
Incubation time 2 h
Animal Experiment
Animal models FaDu, Caki-1, SKOV-3, H460, HT-29, or PAC-120 xenografts in Athymic NMRI-nu/nu female mice
Formulation In a 0.5 % Natrosol solution
Dosages 100 mg/kg
Administration p.o.
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 649.76
Formula C33H39N5O7S
CAS Number 656247-18-6
Purity >99%
Solubility 10 mM in DMSO
Storage at -20°C
References

Safety and pharmacokinetics of nintedanib and pirfenidone in idiopathic pulmonary fibrosis.
Ogura T, et al. Eur Respir J. 2015 May;45(5):1382-92. PMID: 25504994.

Efficacy and safety of nintedanib in idiopathic pulmonary fibrosis.
Richeldi L, et al. N Engl J Med. 2014 May 29;370(22):2071-82. PMID: 24836310.

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Keywords: Nintedanib Ethanesulfonate Salt, BIBF 1120 esylate supplier, VEGFR/PDGFR, inhibitors

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