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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PHA-665752是一种选择性的，ATP竞争性的c-Met抑制剂，IC50为9 nM，对c-Met选择性比RTKs及STKs高50倍以上。
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Foretinib是ATP竞争性HGFR和VEGFR抑制剂，尤其对于Met和KDR抑制性最强，IC50为0.4 nM和0.9 nM，对Ron，Flt-1/3/4，Kit，PDGFRα/β和Tie-2抑制性较弱，而对FGFR1和EGFR则几乎无抑制性。
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Cabozantinib (XL184, BMS-907351)是一种有效的VEGFR2抑制剂，在无细胞试验中IC50为0.035 nM，也能有效抑制c-Met、 Ret、 Kit、Flt-1/3/4、Tie2和AXL，IC50分别为1.3 nM，4 nM，4.6 nM，12 nM/11.3 nM/6 nM，14.3 nM 和 7 nM。
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Crizotinib (PF-02341066)是一种有效的c-Met抑制剂，作用于人的c-Met激酶时，Ki为4 nM。
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PF-04217903是ATP竞争性c-Met抑制剂，IC50为4.8 nM，对突变型Y1230C无活性。
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