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| | MPI-0479605 Basic information |
| Product Name: | MPI-0479605 | | Synonyms: | MPI-0479605;N6-cyclohexyl-N2-(2-methyl-4-morpholinophenyl)-9H-purine-2,6-diamine;MPI0479605 HCl;N6-Cyclohexyl-N2-[2-methyl-4-(4-morpholinyl)phenyl]-9H-purine-2,6-diamine;MPI-0479605;MPI 0479605;MPI0479605;9H-?Purine-?2,?6-?diamine, N6-?cyclohexyl-?N2-?[2-?methyl-?4-?(4-?morpholinyl)?phenyl]?-;CS-1459;MPI-0479605 USP/EP/BP | | CAS: | 1246529-32-7 | | MF: | C22H29N7O | | MW: | 407.51 | | EINECS: | | | Product Categories: | Inhibitors | | Mol File: | 1246529-32-7.mol |  |
| | MPI-0479605 Chemical Properties |
| Boiling point | 745.8±70.0 °C(Predicted) | | density | 1.318±0.06 g/cm3(Predicted) | | storage temp. | Keep in dark place,Inert atmosphere,Store in freezer, under -20°C | | solubility | Soluble in DMSO | | form | A crystalline solid | | pka | 10.52±0.10(Predicted) |
| | MPI-0479605 Usage And Synthesis |
| Description | MPI-0479605 is a potent and ATP-competitive inhibitor of the mitotic kinase MPS1 (IC50 = 1.8 nM). It is selective for MPS1 over a panel of 79 kinases at a concentration of 500 nM. MPI-0479605 induces time-dependent degradation of cyclin B and securin and decreases phosphorylation of BUBR1 resulting in failed cytokinesis in HeLa cells arrested by nocodazole . It also causes misalignment of chromosomes at the anaphase plate and aneuploidy in A549 cells and slows cell cycle progression of HCT116 and COLO 205 cells irrespective of p53 activity. MPI-0479605 (30-150 mg/kg) reduces tumor volume in an HCT116 mouse colon cancer xenograft model in a dose-dependent manner. | | references | [1] tardif k d, rogers a, cassiano j, et al. characterization of the cellular and antitumor effects of mpi-0479605, a small-molecule inhibitor of the mitotic kinase mps1. molecular cancer therapeutics, 2011, 10(12): 2267-2275. |
| | MPI-0479605 Preparation Products And Raw materials |
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