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AMG-458 is a potent and selective inhibitor of human and mouse c-Met with IC50 value of 1.2 nM and 2.0 nM respectively.

c-Met, also known as hepatocyte growth factor receptor, is a receptor tyrosine kinase that can be activated by hepatocyte growth factor/scatter factor (HGF/SF). It is a membrane protein which plays an essential role in embryonic development and wound healing.

Recent study investigated the effect of AMG-456 treatment on cell radiosensitizing response. The results showed that AMG-458 treatment enhanced radiosensitivity in H441 with higher levels of c-Met but not in A549 with lower expression of c-Met [1].

This component was also used in an animal model to study the role of c-Met in the development of tumor. For instance, orally administration of AMG-456 resulted in significant inhibition of tumor growth in /TPR-Met and U-87 MG xenograft models without any adverse effect on body weight [2].

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