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.
| 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 |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
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
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, Checkpoint, Control, Kinases, Monopolar, Spindle, 1, Kinase, Monopolar, Spindle, 1, Kinase, Tocris Bioscience
