SOMCL-863, a novel, selective and orally bioavailable small-molecule c-Met inhibitor, exhibits antitumor activity both in vitro and in vivo
文献类型：期刊论文
| 作者 | Wang, Lu1; Ai, Jing1 ; Shen, Yanyan1; Zhang, Haotian1,4; Peng, Xia1; Huang, Min1; Zhang, Ao2,3; Ding, Jian1; Geng, Meiyu1
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| 刊名 | CANCER LETTERS
 |
| 出版日期 | 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. |
| 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 |
| 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研究方向 | Oncology |
| 语种 | 英语 |
| WOS记录号 | WOS:000339775300018 |
| 出版者 | ELSEVIER IRELAND LTD |
| 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. |
入库方式： OAI收割
来源：上海药物研究所
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