| CAS NO: | 1246529-32-7 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 407.51 |
|---|---|
| Formula | C22H29N7O |
| CAS No. | 1246529-32-7 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 62 mg/mL (152.1 mM) |
| Water:<1 mg/mL | |
| Ethanol: 2 mg/mL (4.9 mM) | |
| Other info | Chemical Name: N6-cyclohexyl-N2-(2-methyl-4-morpholinophenyl)-9H-purine-2,6-diamine InChi Key: OVJBNYKNHXJGSA-UHFFFAOYSA-N InChi Code: InChI=1S/C22H29N7O/c1-15-13-17(29-9-11-30-12-10-29)7-8-18(15)26-22-27-20-19(23-14-24-20)21(28-22)25-16-5-3-2-4-6-16/h7-8,13-14,16H,2-6,9-12H2,1H3,(H3,23,24,25,26,27,28) SMILES Code: CC1=CC(N2CCOCC2)=CC=C1NC3=NC(NC4CCCCC4)=C5N=CNC5=N3 |
| Synonyms | MPI0479605; MPI 0479605; MPI-0479605 |
| In Vitro | In vitro activity: 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. Kinase Assay: To measure Mps1 activity, 25 ng of recombinant, full-length enzyme is incubated in reaction buffer (50 mM Tris-HCl pH 7.5, 10 mM MgCl2, 0.01% Triton X-100 and 5 μM Myelin basic protein (MBP)) containing vehicle (DMSO alone) or inhibitors. Forty μM ATP (2xKm) is added with 1 μCi [γ-33P]ATP and the reaction is incubated at room temperature for 45 minutes. Reactions are terminated with 3% phosphoric acid and transferred to P81 filter plates. Samples are washed in 1% phosphoric acid and 33P radioactivity is measured on a TopCount scintillation reader. In-house kinase assays are all carried out at 2xKm ATP concentrations. MPI-0479605 (500 nM) is also screened against a larger kinase panel. Cell Assay: Cells (A549, Colo205, DU-4475, DU-145, HCC827, HCT116, HT29, MDA MB 231, MiaPaCa2, NCI-H69, NCI-H460, NCI-N87, OPM2, and OVCAR-3 cells.) are treated for 3 or 7 days with various concentrations of MPI-0479605 and the GI50 is determined. Cell viability is measured with CellTiter-Glo. |
|---|---|
| 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. |
| Animal model | Mice bearing subcutaneous HCT-116 or Colo-205 human tumor cell xenografts. |
| Formulation & Dosage | Dissolved in 5% dimethylacetamide (DMA)/12% ethanol/40% PEG-300; daily with 30 mg/kg or every 4 days with 150 mg/kg; i.p. injection |
| References | Mol Cancer Ther. 2011 Dec;10(12):2267-75. |
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