AMG 900

AMG 900 is an orally bioavailable, potent, and highly selective small-molecule inhibitor of aurora kinases A, B, and C. Aurora kinases are crucial regulators of cell division, and their overexpression is associated with poor prognosis and high proliferation in various cancers. AMG 900 works by inhibiting autophosphorylation of aurora-A and -B, as well as phosphorylation of histone H3 on Ser10, leading to aborted cell division and ultimately cell death in tumor cells. It has demonstrated activity in cell lines resistant to taxanes and other aurora kinase inhibitors and was broadly active in preclinical xenograft models, including multidrug-resistant types. Clinically, it was investigated in advanced cancers, including acute myeloid leukemia (AML) and solid tumors, but development has been discontinued[1][3][5][6][7][9].

Other names

N-(4-(3-(2-aminopyrimidin-4-yl)pyridin-2-yloxy)phenyl)-4-(4-methylthiophen-2-yl)phthalazin-1-amine945595-80-2