AZ 3146

Pricing Availability Delivery Time Qty
Cat.No. 3994 - AZ 3146 | C24H32N6O3 | CAS No. 1124329-14-1
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)
Datasheet
Citations (3)
Literature

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.

Compound Libraries

AZ 3146 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 452.55
Formula C24H32N6O3
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 1124329-14-1
PubChem ID 56973724
InChI Key YUKWVHPTFRQHMF-UHFFFAOYSA-N
Smiles CN(C1=CN=C(NC4=CC=C(OC5CCN(C)CC5)C=C4OC)N=C1N2C3CCCC3)C2=O

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.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 452.55. Batch specific molecular weights may vary from batch to batch due to solvent 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
1 mM 2.21 mL 11.05 mL 22.1 mL
5 mM 0.44 mL 2.21 mL 4.42 mL
10 mM 0.22 mL 1.1 mL 2.21 mL
50 mM 0.04 mL 0.22 mL 0.44 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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


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View Related Products by Product Action

View all Monopolar Spindle 1 Kinase Inhibitors

Keywords: 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 Monopolar Spindle 1 Kinase

3 Citations for AZ 3146

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

Karki (2017) Precocious centriole disengagement and centrosome fragmentation induced by mitotic delay. Nat Commun 8 15803 PMID: 28607478

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


Do you know of a great paper that uses AZ 3146 from Tocris? If so please let us know.

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Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
Cell Cycle & DNA Damage Repair

Cell Cycle & DNA Damage Repair Poster

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. Adapted from the 2015 Cancer Product Guide, Edition 3, 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.

Pathways for AZ 3146

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