c-Met
c-Met (tyrosine-protein kinase,HGFR) is a protein that possesses tyrosine kinase activity. The primary single chain precursor protein is post-translationally cleaved to produce the alpha and beta subunits, which are disulfide linked to form the mature receptor. MET is a single pass tyrosine kinase receptor essential for embryonic development, organogenesis and wound healing. Hepatocyte growth factor/Scatter Factor (HGF/SF) and its splicing isoform (NK1, NK2) are the only known ligands of the MET receptor. MET is normally expressed by cells of epithelial origin, while expression of HGF/SF is restricted to cells of mesenchymal origin. When HGF/SF binds its cognate receptor MET it induces its dimerization through a not yet completely understood mechanism leading to its activation.
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SU11274(PKI-SU11274)是Met抑制剂，IC50为10 nM，对PGDFRβ，EGFR和Tie2无活性。
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Tivantinib (ARQ 197)是第一个非ATP竞争性c-Met抑制剂，Ki为355 nM，而对Ron，EGFR，InsR，PDGFRα和FGFR1/4则几乎无抑制性。
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AMG-458是一种有效的c-Met抑制剂，Ki为1.2 nM，作用于c-Met比作用于VEGFR2选择性高350倍左右。
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NVP-BVU972是高活性Met抑制剂，IC50为14 nM，对其它的激酶抑制性较低。
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Golvatinib (E7050)是c-Met和VEGFR-2双重抑制剂，IC50分别为14 nM和16 nM，不抑制bFGF刺激的HUVEC生长(浓度高达1000 nM)。
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