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

doi:10.1111/j.1349-7006.2011.01939.x

CORC > 上海药物研究所 > 中国科学院上海药物研究所 > 药理学第一研究室

	YN968D1 is a novel and selective inhibitor of vascular endothelial growth factor receptor-2 tyrosine kinase with potent activity in vitro and in vivo
	Tian, Shu 1,2; Quan, Haitian3 ; Xie, Chengying3 ; Guo, Haiyi 1,2; Lue, Fangfang 1,2; Xu, Yongping 3; Li, Jin 1,2; Lou, Liguang3
刊名	CANCER SCIENCE
	2011-07
卷号	102 期号:7 页码:1374-1380
ISSN号	1347-9032
DOI	10.1111/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)
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关键词	RENAL-CELL CARCINOMA ; ANTITUMOR-ACTIVITY ; LUNG-CANCER ; VEGF ; BEVACIZUMAB ; THERAPY ; ANGIOGENESIS ; PACLITAXEL ; SORAFENIB ; SU11248
WOS研究方向	Oncology
语种	英语
出版者	WILEY-BLACKWELL
WOS记录号	WOS:000292863100019
内容类型	期刊论文
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.