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Nintedanib (BIBF 1120)

Nintedanib (BIBF 1120) 656247-17-5
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Chemical Information
Product name:Nintedanib (BIBF 1120) Purity:99% min
CAS NO:656247-17-5 Solubility:Soluble in DMSO
Molecular Formula:C31H33N5O4 Package:Packaging according to customer requirements
Molecular Weight:539.62 Storage:Store at -20℃
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Remarks
BIBF 1120 is a potent triple angiokinase inhibitor for VEGFR1/2/3FGFR1/2/3 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 (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)[1].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[1]. BIBF1120 is orally available and displays encouraging efficacy in in vivo tumor models while being well tolerated[2].
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