目錄:MedChemExpress LLC>>生化試劑>> Nintedanib | MCE
CAS | 656247-17-5 | 純度 | 99.85% |
---|---|---|---|
分子量 | 539.62 | 分子式 | C??H??N?O? |
供貨周期 | 現(xiàn)貨 | 規(guī)格 | 5 mg |
貨號 | HY-50904 | 應用領域 | 醫(yī)療衛(wèi)生,化工,生物產業(yè),制藥 |
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CAS No. : 656247-17-5
產品活性:Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
研究領域:Protein Tyrosine Kinase/RTK
作用靶點:PDGFR | VEGFR | FGFR
In Vitro: Nintedanib (BIBF 1120) binds to the ATP-binding site in the cleft between the amino and carboxy terminal lobes of the kinase domain. Nintedanib (BIBF 1120) inhibits proliferation of PDGF-BB stimulated BRPs with EC50 of 79 nM in cell assays. Nintedanib (BIBF 1120) (100 nM) blocks activation of MAPK after stimulation with 5% serum plus PDGF-BB. Nintedanib (BIBF 1120) prevents PDGF-BB stimulated proliferation with an EC50 of 69 nM in cultures of human vascular smooth muscle cells (HUASMC).
In Vivo: Nintedanib (BIBF 1120) (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. Nintedanib (BIBF 1120) is orally available and displays encouraging efficacy in in vivo tumor models while being well tolerated.
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