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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MGCD-265是一种有效的,多靶点,及ATP竞争性的c-Met和VEGFR1/2/3抑制剂,IC50分别为1 nM, 3 nM/3 nM/4 nM,也抑制Ron和Tie2。
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SGX-523是Met抑制剂,IC50为4 nM,对BRAFV599E,c-Raf,Abl和p38α无活性。
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INCB28060是一种新型, ATP竞争性的c-MET抑制剂,IC50为0.13 nM,抑制RONβ, EGFR和HER-3活性。
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EMD 1214063是高活性c-Met选择性抑制剂,IC50为4 nM,比对IRAK4,TrkA,Axl,IRAK1和Mer的抑制性高200倍以上。
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BMS-777607是Met-相关抑制剂,对c-Met,Axl,Ron和Tyro3的IC50分别为3.9 nM,1.1 nM,1.8 nM和4.3 nM,比对Lck,VEGFR-2和TrkA/B的抑制性强40倍。
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