AZ 3146

Cat. No. 3994

AZ 3146 C24H32N6O3 [1124329-14-1]

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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.

Licensing Information

Sold for research purposes only under agreement from AstraZeneca UK Ltd.

Technical Data

Soluble to 25 mM in DMSO and to 75 mM in ethanol
>99 %
Store at +4°C

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.

Certificate of Analysis / Safety Data Sheet

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Safety Data Sheet: View Safety Data Sheet

Hewitt et al (2010) Sustained Mps1 activity is required in mitosis to recruit O-Mad2 to the Mad1-C-Mad2 core complex. J.Cell Biol. 190 25. PMID: 20624899.

Lan and Cleveland (2010) A chemical tool box defines mitotic and interphase roles for Mps1 kinase. J.Cell.Biol. 190 21. PMID: 20624898.

Maciejowski et al (2010) Mps1 directs the assembly of Cdc20 inhbitory complexes during interphase and mitosis to control M phase timing and spindle checkpoint signaling. J.Cell Biol. 190 89. PMID: 20624902.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for AZ 3146 include:

Bennett et al (2015) Cenp-E inhibitor GSK923295: Novel synthetic route and use as a tool to generate aneuploidy. Toxins (Basel) 6 20921. PMID: 26320186.

Hermant et al (2013) Amitozyn impairs chromosome segregation and induces apoptosis via mitotic checkpoint activation. PLoS One 8 e57461. PMID: 23505430.

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Keywords: AZ 3146, supplier, AZ, astrazeneca, Mps1, monopolar, spindle, selective, potent, inhibitors, inhibits, SAC, spindle, assembly, checkpoint, control, TTK, dual-specificity, protein, kinases, kinetochores, CENP-E, centromere, protein, E, AZ3146, Tocris Bioscience, Monopolar Spindle 1 Kinase Inhibitor products

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