MPI-0479605 |
Catalog No.GC10083 |
MPI-0479605 est un puissant inhibiteur compétitif de l'ATP et sélectif de Mps1, avec une IC50 de 1,8 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1246529-32-7
Sample solution is provided at 25 µL, 10mM.
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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