Sunitinib,又称舒尼替尼,是一种ATP竞争性的多靶点受体酪氨酸激酶(RTK)抑制剂,作用于PDGFRβ和VEGFR2的IC50分别为2 nM和80 nM,具有抗肿瘤活性,临床上用于治疗恶性胃肠间质瘤和晚期肾细胞癌。
[1] Sun L, Liang C, Shirazian S, et al. Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosine kinase. J Med Chem. 2003 Mar 27;46(7):1116-9. doi: 10.1021/jm0204183(IF:6.054).
[2] Mendel DB, Laird AD, Xin X, et al. In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship. Clin Cancer Res. 2003 Jan;9(1):327-37(IF:8.911).
[3] O'Farrell AM, Abrams TJ, Yuen HA, et al. SU11248 is a novel FLT3 tyrosine kinase inhibitor with potent activity in vitro and in vivo. Blood. 2003 May 1;101(9):3597-605. doi: 10.1182/blood-2002-07-2307(IF:16.562).
-25~-15℃保存,有效期3年。