VX-680, a potent and selective small-molecule inhibitor of the Aurora kinases, suppresses tumor growth in vivo

摘要: The Aurora kinases are essential for the regulation of chromosome segregation and cytokinesis during mitosis. Aberrant expression activity these occur in a wide range human tumors, lead to aneuploidy tumorigenesis. Here we report discovery highly potent selective small-molecule inhibitor kinases, VX-680, that blocks cell-cycle progression induces apoptosis diverse tumor types. This compound causes profound inhibition growth variety vivo xenograft models, leading regression leukemia, colon pancreatic tumors at well-tolerated doses. Our data indicate kinase provides new approach treatment multiple malignancies.