| 产品描述: | MPS1抑制剂;MPS1 Inhibitors;产品介绍MPI-0479605 是一种有效的,选择性的,ATP 竞争性的 Mps1 抑制剂,IC50 值为 1.8 nM。;InformationMPI-0479605 MPI-0479605 is an ATP competitive and selective inhibitor of mitotic kinase Mps1 with IC50 of 1.8 nM, >40-fold selectivity over other kinases.TargetsMps1 1.8 nMIn vitroMPI-0479605 impairs the SAC and the bipolar attachment of chromosomes to the mitotic spindle, which results in chromosome segregation defects and aneuploidy. MPI-0479605 results in a significant decrease in cell viability with GI50 ranging from 30 to 100 nM in a panel of tumor cell lines. In addition, MPI-0479605 also causes cell growth arrest and ultimately promotes cell death by apoptosis or mitotic catastrophe.In vivoMPI-0479605 (30 mg/kg daily or 150 mg/kg every 4 days, i.p.) shows antitumor activity in colon cancer xenograft models.Cell Research(from reference)Cell lines:A549, Colo205, DU-4475, DU-145, HCC827, HCT116, HT29, MDA MB 231, MiaPaCa2, NCI-H69, NCI-H460, NCI-N87, OPM2, and OVCAR-3 cells. Concentrations:~10 μM Incubation Time:3 or 7 days |