期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 59, 期 6, 页码 2328-2342出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.5b01716
关键词
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Deregulation of the receptor tyrosine kinase mesenchymal epithelial transition factor (MET) has been implicated in several human cancers and is an attractive target for small molecule drug discovery. Herein, we report the discovery of compound 23 (AMG 337), which demonstrates nanomolar inhibition of MET kinase activity, desirable preclinical pharmacokinetics, significant inhibition of MET phosphorylation in mice, and robust tumor growth inhibition in a MET dependent mouse efficacy model.
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