BIBF 1120 esylate,656247-18-6

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YZ剂描述：

产品名称：BIBF 1120 esylate

产品别名：Nintedanib esylate

英文别名：Nintedanib esylate

靶点：FGFR

CAS：656247-18-6

纯度：≥98%

外观：见爱必信官网

保存方法：store at -20℃

描述：

 BIBF 1120 esylate是一种有效的 VEGFR1/2/3，FGFR1/2/3 和 PDGFRα/β 三重YZ剂，IC50 值分别为 34 nM/13 nM/13 nM，69 nM/37 nM/108 nM 和 59 nM/65 nM。

溶解性：DMSO: 92.85 mg/mL

体外研究：

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).

体内研究：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.

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