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。 Information MPI-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. Targets Mps1 1.8 nM In vitro MPI-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 vivo MPI-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
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MPI-0479605
CAS number：1246529-32-7 molecular formula：C22H29N7O
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| Chinese alias | - | ||
| English alias | N6-cyclohexyl-N2-(2-methyl-4-morpholinophenyl)-9H-purine-2,6-diamine | ||
| CAS number | 1246529-32-7 | molecular formula | C22H29N7O |
| molecular weight | 407.51 g/mol | Exact mass | - |
| PSA | 91.000 Ų | logp | 4.379 |
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