SOMCL-863, a novel, selective and orally bioavailable small-molecule c-Met inhibitor, exhibits antitumor activity both in vitro and in vivo.
SOMCL-863, a novel, selective and orally bioavailable small-molecule c-Met inhibitor, exhibits antitumor activity both in vitro and in vivo.
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SOMCL-863 是一种新型、选择性、口服生物可利用的小分子 c-Met 抑制剂，在体外和体内均表现出抗肿瘤活性。
DOI：
10.1016/j.canlet.2014.05.012
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发表时间：
2014-08
期刊：
影响因子：
--
通讯作者：
Geng Meiyu
中科院分区：
文献类型：
--
作者：
Huang Min;Zhang AO;Ding Jian;Geng Meiyu
HGF/c-Met信号的失调及其驱动的肿瘤表型与多种人类恶性肿瘤有关。我们在此报道了SOMCL-863作为一种新的选择性c-Met抑制剂，它有效地破坏了c-Met信号通路，从而导致c-Met依赖性细胞增殖、迁移、侵袭、细胞散射和侵袭性生长的实质性损害。在EBC-1和NCI-H1993异种移植物中，SOMCL-863通过抑制肿瘤细胞增殖、降低微血管密度和促血管生成因子IL-8的分泌等抗增殖和抗血管生成机制发挥了显著的抗肿瘤作用。SOMCL-863具有最佳的药代动力学特性，值得进一步评估其作为c- met驱动的人类癌症的治疗方法。
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.
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影响因子：
7.3
作者：
Yuanxiang Wang;Jing Ai;Ying Wang;Yi Chen;Lu Wang;Gang Liu;M. Geng;Ao Zhang
通讯作者：
Yuanxiang Wang;Jing Ai;Ying Wang;Yi Chen;Lu Wang;Gang Liu;M. Geng;Ao Zhang
影响因子：
11.2
作者：
G. Dong;Zhong Chen;Zhi-yu Li;N. Yeh;C. Bancroft;C. Waes
通讯作者：
G. Dong;Zhong Chen;Zhi-yu Li;N. Yeh;C. Bancroft;C. Waes
DOI：
10.1073/pnas.0508776103
发表时间：
2006-02-14
影响因子：
11.1
作者：
Smolen, GA;Sordella, R;Haber, DA
通讯作者：
Haber, DA
影响因子：
8.2
作者：
Wang, Xiao-lei;Chen, Xi-mei;Yang, Chang-qin
通讯作者：
Yang, Chang-qin
影响因子：
8.2
作者：
He, Chang-xi;Ai, Jing;Geng, Mei-yu
通讯作者：
Geng, Mei-yu