永利3044(中国集团)有限公司官网

_{Sunitinib Malate是多靶点受体酪氨酸激酶(RTK)抑制剂，抑制VEGFR2和PDGFR β活性，无细胞实验中检测IC50值分别为80 nM和2 nM。Sunitinib Malate还会抑制c-Kit的活性，IC50值为211 nM。除此之外，Sunitinib Malate还是一种有效的ATP竞争性抑制剂，可通过抑制自身磷酸化和激活RNase来有效抑制Ire1α的磷酸化，达到有效抑制肿瘤细胞增殖，诱导细胞凋亡的目的。}

参考文献

[1] Sun L, 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, 46 (7), 1116-1119.

[2] O'Farrell AM, et al. SU11248 is a novel FLT3 tyrosine kinase inhibitor with potent activity in vitro and in vivo. Blood, 2003, 101(9), 3597-3605.

[3] Mendel DB, 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, 9(1), 327-337.

冰袋运输。粉末-20 ℃保存，3年有效；4 ℃保存，2年有效。储存液-80 ℃保存，6个月有效；-20 ℃保存，1个月有效。