MPI-0479605Mps1 inhibitor,selective and ATP competitive CAS# 1246529-32-7 |
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Quality Control & MSDS
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| Cas No. | 1246529-32-7 | SDF | Download SDF |
| PubChem ID | 46909588 | Appearance | Powder |
| Formula | C22H29N7O | M.Wt | 407.51 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : 11 mg/mL (26.99 mM; Need ultrasonic and warming) | ||
| Chemical Name | 6-N-cyclohexyl-2-N-(2-methyl-4-morpholin-4-ylphenyl)-7H-purine-2,6-diamine | ||
| SMILES | CC1=C(C=CC(=C1)N2CCOCC2)NC3=NC4=C(C(=N3)NC5CCCCC5)NC=N4 | ||
| Standard InChIKey | OVJBNYKNHXJGSA-UHFFFAOYSA-N | ||
| Standard InChI | 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) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | MPI-0479605 is a novel small-molecule inhibitor of the Mitotic kinase Mps1 with IC50 value of 1.8 nM. | |||||
| Targets | Mps1 | |||||
| IC50 | 1.8 nM | |||||
MPI-0479605 Dilution Calculator
MPI-0479605 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.4539 mL | 12.2696 mL | 24.5393 mL | 49.0786 mL | 61.3482 mL |
| 5 mM | 0.4908 mL | 2.4539 mL | 4.9079 mL | 9.8157 mL | 12.2696 mL |
| 10 mM | 0.2454 mL | 1.227 mL | 2.4539 mL | 4.9079 mL | 6.1348 mL |
| 50 mM | 0.0491 mL | 0.2454 mL | 0.4908 mL | 0.9816 mL | 1.227 mL |
| 100 mM | 0.0245 mL | 0.1227 mL | 0.2454 mL | 0.4908 mL | 0.6135 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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MPI-0479605 is a small-molecule inhibitor of the Mitotic Kinase Mps1 with IC50 value of 1.8nM [1].
MPI-0479605 is a selective and ATP competitive inhibitor of Mps1. It shows no significant inhibition of 120 other kinases. In cells treated with nocodazole, MPI-0479605 inhibits Mps1 function through promoting the degradation of both cyclin B and securing. MPI-0479605 also suppresses the autophosphorylation of Mps1 in HEK293T cells overexpressing this enzyme. In A549 cells during mitosis, MPI-0479605 causes defects in chromosome segregation. It destroys the ability of cells to align chromosomes at the metaphase plate. Besides that, MPI-0479605-treated cells also show a significant delay or arrest in cell-cycle progression. Moreover, treatment of MPI-0479605 leads to a significant decrease in cell viability in HCT-116 cells and finally causes cell death with GI50 values ranging from 30nM to 100nM. Furthermore, MPI-0479605 shows potent antitumor effects in tumor xenograft models. MPI-0479605 at dose of 30mg/kg results in TGI of 49% in mice bearing HCT-116 xenografts [1].
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.
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Characterization of the cellular and antitumor effects of MPI-0479605, a small-molecule inhibitor of the mitotic kinase Mps1.[Pubmed:21980130]
Mol Cancer Ther. 2011 Dec;10(12):2267-75.
Mps1 is a dual specificity protein kinase that is essential for the bipolar attachment of chromosomes to the mitotic spindle and for maintaining the spindle assembly checkpoint until all chromosomes are properly attached. Mps1 is expressed at high levels during mitosis and is abundantly expressed in cancer cells. Disruption of Mps1 function induces aneuploidy and cell death. We report the identification of MPI-0479605, a potent and selective ATP competitive inhibitor of Mps1. Cells treated with MPI-0479605 undergo aberrant mitosis, resulting in aneuploidy and formation of micronuclei. In cells with wild-type p53, this promotes the induction of a postmitotic checkpoint characterized by the ATM- and RAD3-related-dependent activation of the p53-p21 pathway. In both wild-type and p53 mutant cells lines, there is a growth arrest and inhibition of DNA synthesis. Subsequently, cells undergo mitotic catastrophe and/or an apoptotic response. In xenograft models, MPI-0479605 inhibits tumor growth, suggesting that drugs targeting Mps1 may have utility as novel cancer therapeutics.
