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Submit ReviewAZ 3146
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)
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 |
| 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.
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 | |
|---|---|---|---|
| Solubility | |||
| 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.
| 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
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.
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13 Citations for AZ 3146
Citations are publications that use Tocris products. Selected citations for AZ 3146 include:
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
Joana C et al (2020) Small-molecule inhibition of aging-associated chromosomal instability delays cellular senescence. EMBO Rep 21 e49248 PMID: 32134180
Shabaz et al (2020) Ordered dephosphorylation initiated by the selective proteolysis of cyclin B drives mitotic exit. Elife 9 PMID: 32869743
Haase et al (2017) Distinct Roles of the Chromosomal Passenger Complex in the Detection of and Response to Errors in Kinetochore-Microtubule Attachment. Dev Cell 42 640 PMID: 28950102
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
Drpic et al (2018) Chromosome Segregation Is Biased by Kinetochore Size. Curr Biol 28 1344 PMID: 29706521
McKinley et al (2018) Cellular aspect ratio and cell division mechanics underlie the patterning of cell progeny in diverse mammalian epithelia. Elife 7 PMID: 29897330
Jun et al (2021) Separase cleaves the kinetochore protein Meikin at the meiosis I/II transition. Dev Cell 56 2192-2206.e8 PMID: 34331869
Littler et al (2019) Oncogenic MYC amplifies mitotic perturbations. Open Biol 9 190136 PMID: 31455158
Karki (2017) Precocious centriole disengagement and centrosome fragmentation induced by mitotic delay. Nat Commun 8 15803 PMID: 28607478
Do you know of a great paper that uses AZ 3146 from Tocris? Please let us know.
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Cell Cycle and DNA Damage Research Product Guide
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