Nintedanib(BIBF 1120; Intedanib)是一种受体酪氨酸激酶VEGFR/FGFR/PDGFR的抑制剂,对VEGFR1/2/3的IC50值分别是34 nM/13 nM/13 nM,对FGFR1/2/3的IC50值分别是69 nM/37 nM/108 nM,对PDGFRα/β的IC50值分别是59 nM/65 nM。 Nintedanib(BIBF 1120; Intedanib)靶向血小板源生长因子受体(PDGFα/β)、纤维母细胞生长因子受体(FGFR1/2/3)、血管内皮生长因子受体(VEGFR1/2/3),与这些受体的三磷酸腺苷(ATP)结合位点竞争性结合,阻断纤维化进程的信号通路,抑制纤维母细胞的扩散、转移和转变,从而减缓特发性肺纤维化的疾病进程。
参考文献
[1]. Tai W T, et al. Nintedanib (BIBF-1120) inhibits hepatocellular carcinoma growth independent of angiokinase activity. Journal of hepatology, 2014.
[2]. Cenik B K, et al. BIBF 1120 (nintedanib), a triple angiokinase inhibitor, induces hypoxia but not EMT and blocks progression of preclinical models of lung and pancreatic cancer. Molecular cancer therapeutics, 2013, 12(6): 992-1001.
冰袋运输。粉末直接保存于-20℃,有效期2年。溶于DMSO。建议分装后-20℃避光保存,避免反复冻融。