AZ 3146

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Description: Potent and selective Mps1 kinase inhibitor
Chemical Name: 9-Cyclopentyl-2-[[2-methoxy-4-[(1-methylpiperidin-4-yl)oxy]-phenyl]amino]-7-methyl-7,9-dihydro-8H-purin-8-one
Purity: ≥99% (HPLC)
Citations (13)
Literature (2)

Biological Activity for AZ 3146

AZ 3146 is a 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.

Compound Libraries for AZ 3146

AZ 3146 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.

Technical Data for AZ 3146

M. Wt 452.55
Formula C24H32N6O3
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 1124329-14-1
PubChem ID 56973724

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for AZ 3146

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 11.31 25
ethanol 33.94 75

Preparing Stock Solutions for AZ 3146

The following data is based on the product molecular weight 452.55. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.75 mM 2.95 mL 14.73 mL 29.46 mL
3.75 mM 0.59 mL 2.95 mL 5.89 mL
7.5 mM 0.29 mL 1.47 mL 2.95 mL
37.5 mM 0.06 mL 0.29 mL 0.59 mL

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Product Datasheets for AZ 3146

Certificate of Analysis / Product Datasheet
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References for AZ 3146

References are publications that support the biological activity of the product.

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 AZ 3146, please let us know.

View Related Products by Product Action

View all Monopolar Spindle 1 Kinase Inhibitors

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13 Citations for AZ 3146

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

Littler et al (2019) Oncogenic MYC amplifies mitotic perturbations. Open Biol 9 190136 PMID: 31455158

Iain M et al (2017) Large-Scale Analysis of CRISPR/Cas9 Cell-Cycle Knockouts Reveals the Diversity of p53-Dependent Responses to Cell-Cycle Defects. Dev Cell 40 405-420.e2 PMID: 28216383

Jing et al (2018) Methods for High-throughput Drug Combination Screening and Synergy Scoring. Methods Mol Biol 1711 351-398 PMID: 29344898

Garvanska et al (2016) Synergistic inhibition of the APC/C by the removal of APC15 in HCT116 cells lacking UBE2C. Biol Open 5 1441 PMID: 27591192

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Literature in this Area

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Cell Cycle and DNA Damage Research Product Guide

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In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. This poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.