Catalog Number: 2458
Chemical Name: N-[4-[[6-Methoxy-7-[3-(4-morpholinyl)propoxy]-4-quinazolinyl]amino]phenyl]benzamide
Biological Activity
Novel, selective ATP-competitive inhibitor of Aurora B kinase in vitro (IC50 values are 50, 250 and 1000 nM for Aurora B, C and A kinases respectively). Selective over a range of other kinases including cdk1 and PLK1 (IC50 > 10 μM). Inhibits cell division and displays selective toxicity towards proliferating tumor cells versus non-dividing cells.
Technical Data
  • M.Wt:
    513.59
  • Formula:
    C29H31N5O4
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at -20°C
  • CAS No:
    331771-20-1
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.
Additional Information
Licensing Caveats:
Sold with the permission of AstraZeneca UK Ltd.
Background References
  1. Aurora B couples chromosome alignment with anaphase by targeting BubR1, Mad2, and Cenp-E to kinetochores.
    Ditchfield et al.
    J.Cell Biol., 2003;161:267
  2. Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors.
    Jung et al.
    J.Med.Chem., 2006;49:955
  3. Validating Aurora B as an anti-cancer drug target.
    Girdler et al.
    J.Cell Sci., 2006;119:3664
Citations:

The citations listed below are publications that use Tocris products. Selected citations for ZM 447439 include:

26 Citations: Showing 1 - 10
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  1. Aurora-B kinase pathway controls the lateral to end-on conversion of kinetochore-microtubule attachments in human cells.
    Authors: Shrestha
    Nat Commun 2017;8(1):150
  2. Stable kinetochore-microtubule attachment is sufficient to silence the spindle assembly checkpoint in human cells.
    Authors: Tauchman Et al.
    J Cell Sci 2015;6:10036
  3. Mio depletion links mTOR regulation to Aurora A and Plk1 activation at mitotic centrosomes.
    Authors: Platani Et al.
    J Cell Biol 2015;210:45
  4. Multiple assembly mechanisms anchor the KMN spindle checkpoint platform at human mitotic kinetochores.
    Authors: Kim and Yu
    J Cell Biol 2015;208:181
  5. Centmitor-1, a novel acridinyl-acetohydrazide, possesses similar molecular interaction field and antimitotic cellular phenotype as rigosertib, on 01910.Na.
    Authors: Mäki-Jouppila Et al.
    Nat Commun 2014;13:1054
  6. Selective disruption of aurora C kinase reveals distinct functions from aurora B kinase during meiosis in mouse oocytes.
    Authors: Balboula and Schindler
    PLoS Genet 2014;10:e1004194
  7. Aurora B spatially regulates EB3 phosphorylation to coordinate daughter cell adhesion with cytokinesis.
    Authors: Ferreira Et al.
    J Cell Biol 2013;201:709
  8. Spatiotemporal organization of Aurora-B by APC/CCdh1 after mitosis coordinates cell spreading through FHOD1.
    Authors: Floyd Et al.
    Cell Cycle 2013;126:2845
  9. Haspin inhibitors reveal centromeric functions of Aurora B in chromosome segregation.
    Authors: Wang Et al.
    J Cell Biol 2012;199:251
  10. Aurora kinase B activity is modulated by thyroid hormone during transcriptional activation of pituitary genes.
    Authors: Tardáguila Et al.
    Mol Endocrinol 2011;25:385
  11. Zwint-1 is a novel Aurora B substrate required for the assembly of a dynein-binding platform on kinetochores.
    Authors: Kasuboski Et al.
    Mol Biol Cell 2011;22:3318
  12. Polo-box domain inhibitor poloxin activates the spindle assembly checkpoint and inhibits tumor growth in vivo.
    Authors: Yuan Et al.
    Am J Pathol 2011;179:2091
  13. Formation of stable attachments between kinetochores and microtubules depends on the B56-PP2A phosphatase.
    Authors: Foley Et al.
    Nat Cell Biol 2011;13:1265
  14. Role of a novel coiled-coil domain-containing protein CCDC69 in regulating central spindle assembly.
    Authors: Pal Et al.
    J Am Soc Nephrol 2010;9:4117
  15. VHL inactivation induces HEF1 and Aurora kinase A.
    Authors: Xu Et al.
    J Cell Biol 2010;21:2041
  16. Relocation of the chromosomal passenger complex prevents mitotic checkpoint engagement at anaphase.
    Authors: Vázquez-Novelle and Petronczki
    Curr Biol 2010;20:1402
  17. Plk1 negatively regulates Cep55 recruitment to the midbody to ensure orderly abscission.
    Authors: Bastos and Barr
    J Cell Biol 2010;191:751
  18. Release of Mps1 from kinetochores is crucial for timely anaphase onset.
    Authors: Jelluma Et al.
    Cell Cycle 2010;191:281
  19. Epigenetic centromere specification directs aurora B accumulation but is insufficient to efficiently correct mitotic errors.
    Authors: Bassett Et al.
    Mol Cancer Ther 2010;190:177
  20. Targeting mitotic exit leads to tumor regression in vivo: Modulation by Cdk1, Mastl, and the PP2A/B55α,δ phosphatase.
    Authors: Manchado Et al.
    Cancer Cell 2010;18:641
  21. Human condensin function is essential for centromeric chromatin assembly and proper sister kinetochore orientation.
    Authors: Samoshkin Et al.
    PLoS One 2009;4:e6831
  22. Discovery and exploitation of inhibitor-resistant aurora and polo kinase mutants for the analysis of mitotic networks.
    Authors: Scutt Et al.
    J Biol Chem 2009;284:15880
  23. The Nup107-160 nucleoporin complex promotes mitotic events via control of the localization state of the chromosome passenger complex.
    Authors: Platani Et al.
    Mol Biol Cell 2009;20:5260
  24. Cell cycle dependent degradation of MCAK: evidence against a role in anaphase chromosome movement.
    Authors: Ganguly Et al.
    Toxins (Basel) 2008;7:3187
  25. A mitotic GlcNAcylation/phosphorylation signaling complex alters the posttranslational state of the cytoskeletal protein vimentin.
    Authors: Slawson Et al.
    Mol Biol Cell 2008;19:4130
  26. Frequent overexpression of aurora B kinase, a novel drug target, in non-small cell lung carcinoma patients.
    Authors: Vischioni Et al.
    Mol Cancer Ther 2006;5:2905
Expand to show all 26 Citations

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