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BIBF 1120 is an effective triple vascular kinase inhibitor that inhibits VEGFR1/2/3, FGFR1/2/3, and PDGFR α/β  The IC50 values are 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM, and 59 nM/65 nM, respectively.
Related categories
Signal Pathways>>Protein Tyrosine Kinases>>FGFR
Signal Pathways>>Protein Tyrosine Kinases>>PDGFR
Signal Pathways>>Protein Tyrosine Kinases>>VEGFR
Research Fields>>Cancer
Target point
VEGFR1:34 nM (IC50)
VEGFR2:13 nM (IC50)
VEGFR3:13 nM (IC50)
FGFR1:69 nM (IC50)
FGFR2:37 nM (IC50)
FGFR3:108 nM (IC50)
PDGFR α: 59 nM (IC50)
PDGFR β: 65 nM (IC50)
In vitro study of the ATP binding sites in the gap between the amino and carboxyl terminal fragments of the BIBF 1120 binding kinase domain. BIBF 1120 inhibits the proliferation of PDGF-BB stimulated BRP in cell assays, with an EC50 of 79nM. After stimulation with 5% serum and PDGF-BB, BIBF1120 (100nM) blocked the activation of MAPK. BIBF1120 can prevent PDGF-BB from stimulating proliferation, with an EC50 of 69 nM in human vascular smooth muscle cell (HUASMC) culture.
In vivo studies have shown that BIBF1120 (25-100mg/kg orally administered daily) exhibits high activity in all tumor models, including human tumor xenografts grown in nude mice and homologous rat tumor models. This is evident in the magnetic resonance imaging of tumor perfusion after 3 days, with a decrease in vascular density and integrity after 5 days, and severe inhibition of growth [1]. BIBF1120 can be orally administered and has shown encouraging efficacy in vivo tumor models, while also exhibiting good tolerance [2].
The kinase experiment measured enzyme activity in the presence or absence of continuous dilution of BIBF1120 in 25% DMSO. Each micro titration plate contains internal controls such as blank, maximum reaction, and historical reference compounds. All incubation was conducted at room temperature on a rotating oscillator. Add 10 μ Add 10 to each BIBF1120 diluent μ L-diluted kinase (0.8 μ G/mL VEGFR2,10mM Tris pH 7.5,2mM EDTA and 2mg/mL BSA) and pre incubate for 1 hour. By adding 30 μ L contains 62.4mM Tris pH 7.5,2.7mM DTT, 5.3mM MnCl 2,13.3mM