Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor forVEGFR1/2/3,FGFR1/2/3andPDGFRα/βwithIC₅₀s 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. Nintedanib (BIBF 1120) inhibits proliferation of PDGF-BB stimulated BRPs with EC₅₀of 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 EC₅₀of 69 nM in cultures of human vascular smooth muscle cells (HUASMC)^[1].

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^[1]. Nintedanib (BIBF 1120) is orally available and displays encouraging efficacy in in vivo tumor models while being well tolerated^[2].

539.62

Solid

C₃₁H₃₃N₅O₄

656247-17-5

尼达尼布

Room temperature in continental US; may vary elsewhere.

DMSO : 11.5 mg/mL(21.31 mM;Need ultrasonic)

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