| MPI-0479605Mps1 inhibitor,selective and ATP competitive |
Sample solution is provided at 25 µL, 10mM.
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- Purity = 98.00%
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Chemical structure
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| 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 | |||||
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| Cas No. | 1246529-32-7 | SDF | Download SDF |
| Canonical SMILES | CC1=C(C=CC(=C1)N2CCOCC2)NC3=NC4=C(C(=N3)NC5CCCCC5)NC=N4 | ||
| Formula | C22H29N7O | M.Wt | 407.51 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request | ||
| 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. | ||
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.
