生化机理 |
AMG 900 is a novel potent and highly selective Pan-aurora kinase inhibitor with an IC50 of median 3.5 nM. AMG 900 repressed autophosphorylation of aurorakinases A and B as well as the phosphorylation of histone H3.The predominant cellular response of tumor cells to AMG 900treatment is aborted cell division without a mitotic arrest, which leads to endoreduplication and cell death. AMG 900 was originally developed by Amgen. A phase 1 first-in-human study evaluating AMG 900 in advanced solid tumors is currently recruiting participants. |