SOMCL-863, a novel, selective and orally bioavailable small-molecule c-Met inhibitor, exhibits antitumor activity both in vitro and in vivo

doi:10.1016/j.canlet.2014.05.012

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	SOMCL-863, a novel, selective and orally bioavailable small-molecule c-Met inhibitor, exhibits antitumor activity both in vitro and in vivo
	Wang, Lu 1; Ai, Jing1 ; Shen, Yanyan 1; Zhang, Haotian 1,4; Peng, Xia 1; Huang, Min1 ; Zhang, Ao2,3 ; Ding, Jian1 ; Geng, Meiyu1
刊名	CANCER LETTERS
	2014-08-28
卷号	351 期号:1 页码:143-150
关键词	c-Met SOMCL-863 Receptor tyrosine kinase Cancer Angiogenesis
ISSN号	0304-3835
DOI	10.1016/j.canlet.2014.05.012
文献子类	Article
英文摘要	Deregulation of HGF/c-Met signaling and its driven neoplastic phenotype are associated with a variety of human malignancies. We herein reported SOMCL-863 as a novel selective c-Met inhibitor which effectively abrogated c-Met signaling pathways, thereby leading to substantial impairment of c-Met-dependent cell proliferation, migration, invasion, cell scattering and invasive growth. In EBC-1 and NCI-H1993 xenografts, SOMCL-863 exerted significant anti-tumor efficacy through anti-proliferative effects and antiangiogenic mechanisms, including reduction of tumor cell proliferation and reductions of microvessel density and secretion of proangiogenic factor IL-8. Together with the optimal pharmacokinetic properties, SOMCL-863 is a promising candidate worthy for further evaluation as a treatment of c-Met-driven human cancers. (C) 2014 Elsevier Ireland Ltd. All rights reserved.
资助项目	National Program on Key Basic Research Project of China[2012CB910704] ; National Natural Science Foundation[91229205] ; National Natural Science Foundation[81102461] ; National Natural Science Foundation[81321092] ; National S&T Major Projects[2012ZX09301001-007]
WOS关键词	EPITHELIAL-MESENCHYMAL TRANSITIONS ; ENDOTHELIAL GROWTH-FACTOR ; RECEPTOR TYROSINE KINASE ; LUNG-CANCER ; SCATTER FACTOR ; THERAPEUTIC INHIBITION ; TUMOR PROGRESSION ; INVASIVE GROWTH ; GASTRIC-CANCER ; AMPLIFICATION
WOS研究方向	Oncology
语种	英语
出版者	ELSEVIER IRELAND LTD
WOS记录号	WOS:000339775300018
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/276934]
专题	药理学第一研究室中科院受体结构与功能重点实验室新药研究国家重点实验室药物化学研究室
通讯作者	Ding, Jian
作者单位	1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Div Antitumor Pharmacol, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, Shanghai 201203, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, Synthet Organ & Med Chem Lab SOMCL, Shanghai 201203, Peoples R China; 4.Shenyang Pharmaceut Univ, Dept Pharmacol, Shenyang 110016, Peoples R China
推荐引用方式 GB/T 7714	Wang, Lu,Ai, Jing,Shen, Yanyan,et al. SOMCL-863, a novel, selective and orally bioavailable small-molecule c-Met inhibitor, exhibits antitumor activity both in vitro and in vivo[J]. CANCER LETTERS,2014,351(1):143-150.
APA	Wang, Lu.,Ai, Jing.,Shen, Yanyan.,Zhang, Haotian.,Peng, Xia.,...&Geng, Meiyu.(2014).SOMCL-863, a novel, selective and orally bioavailable small-molecule c-Met inhibitor, exhibits antitumor activity both in vitro and in vivo.CANCER LETTERS,351(1),143-150.
MLA	Wang, Lu,et al."SOMCL-863, a novel, selective and orally bioavailable small-molecule c-Met inhibitor, exhibits antitumor activity both in vitro and in vivo".CANCER LETTERS 351.1(2014):143-150.