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YN968D1 is a novel and selective inhibitor of vascular endothelial growth factor receptor-2 tyrosine kinase with potent activity in vitro and in vivo

文献类型：期刊论文

作者Tian, Shu1,2; Quan, Haitian3; Xie, Chengying3; Guo, Haiyi1,2; Lue, Fangfang1,2; Xu, Yongping3; Li, Jin1,2; Lou, Liguang3
刊名CANCER SCIENCE
出版日期2011-07
卷号102期号:7页码:1374-1380
ISSN号1347-9032
DOI10.1111/j.1349-7006.2011.01939.x
文献子类Article
英文摘要Angiogenesis is an important process in cell development, especially in cancer. Vascular endothelial growth factor (VEGF) signaling is an important regulator of angiogenesis. Several therapies that act against VEGF signal transduction have been developed, including YN968D1, which is a potent inhibitor of the VEGF signaling pathway. This study investigated the antitumor activity of YN968D1 (apatinib mesylate) in vitro and in vivo. YN968D1 potently suppressed the kinase activities of VEGFR-2, c-kit and c-src, and inhibited cellular phosphorylation of VEGFR-2, c-kit and PDGFR beta. YN968D1 effectively inhibited proliferation, migration and tube formation of human umbilical vein endothelial cells induced by FBS, and blocked the budding of rat aortic ring. In vivo, YN968D1 alone and in combination with chemotherapeutic agents effectively inhibited the growth of several established human tumor xenograft models with little toxicity. A phase I study of YN968D1 has shown encouraging antitumor activity and a manageable toxicity profile. These findings suggest that YN968D1 has promise as an antitumor drug and might have clinical benefits. (Cancer Sci 2011; 102: 1374-1380)
WOS关键词RENAL-CELL CARCINOMA ; ANTITUMOR-ACTIVITY ; LUNG-CANCER ; VEGF ; BEVACIZUMAB ; THERAPY ; ANGIOGENESIS ; PACLITAXEL ; SORAFENIB ; SU11248
资助项目National Natural Science Foundation of China[90813009] ; National Science and Technology Major Project "Key New Drug Creation and Manufacturing Program"[2009ZX09102-022]
WOS研究方向Oncology
语种英语
WOS记录号WOS:000292863100019
出版者WILEY-BLACKWELL
源URL[http://119.78.100.183/handle/2S10ELR8/278483]  
专题药理学第一研究室
通讯作者Li, Jin
作者单位1.Fudan Univ, Dept Med Oncol, Shanghai Canc Ctr, Shanghai 200433, Peoples R China;
2.Fudan Univ, Dept Oncol, Shanghai Med Coll, Shanghai 200433, Peoples R China;
3.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 200031, Peoples R China
推荐引用方式
GB/T 7714		 Tian, Shu,Quan, Haitian,Xie, Chengying,et al. YN968D1 is a novel and selective inhibitor of vascular endothelial growth factor receptor-2 tyrosine kinase with potent activity in vitro and in vivo[J]. CANCER SCIENCE,2011,102(7):1374-1380.
APA Tian, Shu.,Quan, Haitian.,Xie, Chengying.,Guo, Haiyi.,Lue, Fangfang.,...&Lou, Liguang.(2011).YN968D1 is a novel and selective inhibitor of vascular endothelial growth factor receptor-2 tyrosine kinase with potent activity in vitro and in vivo.CANCER SCIENCE,102(7),1374-1380.
MLA Tian, Shu,et al."YN968D1 is a novel and selective inhibitor of vascular endothelial growth factor receptor-2 tyrosine kinase with potent activity in vitro and in vivo".CANCER SCIENCE 102.7(2011):1374-1380.

入库方式： OAI收割

来源：上海药物研究所

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