Catalog Number: 3994
Chemical Name: 9-Cyclopentyl-2-[[2-methoxy-4-[(1-methylpiperidin-4-yl)oxy]-phenyl]amino]-7-methyl-7,9-dihydro-8H-purin-8-one
Biological Activity
Potent and selective monopolar spindle 1 (Mps1) kinase inhibitor (IC50 = 35 nM). Displays selectivity over 46 other kinases including Cdk1 and aurora kinase B. Interferes with chromosome alignment and overrides spindle assembly checkpoint. Inhibits the recruitment of Mad1, Mad2 and centromere protein E (CENP-E) to kinetochores.
Technical Data
  • M.Wt:
    452.55
  • Formula:
    C24H32N6O3
  • Solubility:
    Soluble to 25 mM in DMSO and to 75 mM in ethanol
  • Purity:
    >99%
  • Storage:
    Store at +4°C
  • CAS No:
    1124329-14-1
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Additional Information
Licensing Caveats:
Sold for research purposes only under agreement from AstraZeneca UK Ltd.
Background References
  1. Sustained Mps1 activity is required in mitosis to recruit O-Mad2 to the Mad1-C-Mad2 core complex.
    Hewitt et al.
    J.Cell Biol., 2010;190:25
  2. A chemical tool box defines mitotic and interphase roles for Mps1 kinase.
    Lan and Cleveland
    J.Cell.Biol., 2010;190:21
  3. Mps1 directs the assembly of Cdc20 inhbitory complexes during interphase and mitosis to control M phase timing and spindle checkpoint signaling.
    Maciejowski et al.
    J.Cell Biol., 2010;190:89
Citations:

The citations listed below are publications that use Tocris products. Selected citations for AZ 3146 include:

3 Citations: Showing 1 - 3
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  1. Precocious centriole disengagement and centrosome fragmentation induced by mitotic delay.
    Authors: Karki
    Nat Commun 2017;8:15803
  2. Cenp-E inhibitor GSK923295: Novel synthetic route and use as a tool to generate aneuploidy.
    Authors: Bennett Et al.
    Toxins (Basel) 2015;6:20921
  3. Amitozyn impairs chromosome segregation and induces apoptosis via mitotic checkpoint activation.
    Authors: Hermant Et al.
    PLoS One 2013;8:e57461

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