ZM 447439

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2458/10
ZM 447439 | CAS No. 331771-20-1 | Aurora Kinase Inhibitors
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Description: Inhibits Aurora kinase B

Chemical Name: N-[4-[[6-Methoxy-7-[3-(4-morpholinyl)propoxy]-4-quinazolinyl]amino]phenyl]benzamide

Purity: ≥98%

Product Details
Citations (49)
Reviews

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

Additional Information

Licensing Caveats:
Sold with the permission of AstraZeneca UK Ltd.

Product Datasheets

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Citations for ZM 447439

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

49 Citations: Showing 1 - 10

  1. Oncogenic MYC amplifies mitotic perturbations.
    Authors: Littler Et al.
    Open Biol  2019;9:190136
  2. Spatiotemporal control of mitotic exit during anaphase by an aurora B-Cdk1 crosstalk.
    Authors: Afonso Et al.
    Elife  2019;8
  3. Interactions between N-terminal Modules in MPS1 Enable Spindle Checkpoint Silencing.
    Authors: Pachis Et al.
    Cell Rep  2019;26:2101
  4. Lipid accumulation facilitates mitotic slippage-induced adaptation to anti-mitotic drug treatment.
    Authors: Wong Et al.
    Cell Death Discov  2018;4:109
  5. Atypical Cadherin Dachsous1b Interacts with Ttc28 and Aurora B to Control Microtubule Dynamics in Embryonic Cleavages.
    Authors: Chen Et al.
    Dev Cell  2018;45:376
  6. Dynamic kinetochore size regulation promotes microtubule capture and chromosome biorientation in mitosis.
    Authors: Sacristan Et al.
    Nat Cell Biol  2018;20:800
  7. Mps1 kinase-dependent Sgo2 centromere localisation mediates cohesin protection in mouse oocyte meiosis I.
    Authors: Yakoubi Et al.
    Nat Commun  2017;8:694
  8. 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
  9. Distinct Roles of the Chromosomal Passenger Complex in the Detection of and Response to Errors in Kinetochore-Microtubule Attachment.
    Authors: Haase Et al.
    Dev Cell  2017;42:640
  10. Haspin inhibition reveals functional differences of interchromatid axis-localized AURKB and AURKC.
    Authors: Quartuccio Et al.
    Mol Biol Cell  2017;28:2233
  11. Ska3 Phosphorylated by Cdk1 Binds Ndc80 and Recruits Ska to Kinetochores to Promote Mitotic Progression.
    Authors: Zhang Et al.
    Curr Biol  2017;27:1477
  12. Baculoviral delivery of CRISPR/Cas9 facilitates efficient genome editing in human cells.
    Authors: Hindriksen Et al.
    PLoS One  2017;12:e0179514
  13. Kif4 Is Essential for Mouse Oocyte Meiosis.
    Authors: Camlin Et al.
    PLoS One  2017;12:e0170650
  14. Aurora-A mediated histone H3 phosphorylation of threonine 118 controls condensin I and cohesin occupancy in mitosis.
    Authors: Wike Et al.
    Elife  2016;5:e11402
  15. Haspin kinase regulates microtubule-organizing center clustering and stability through Aurora kinase C in mouse oocytes.
    Authors: Balboula Et al.
    J Cell Sci  2016;129:3648
  16. 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
  17. Mio depletion links mTOR regulation to Aurora A and Plk1 activation at mitotic centrosomes.
    Authors: Platani Et al.
    J Cell Biol  2015;210:45
  18. Multiple assembly mechanisms anchor the KMN spindle checkpoint platform at human mitotic kinetochores.
    Authors: Kim and Yu
    J Cell Biol  2015;208:181
  19. Phosphorylation of myosin II-interacting guanine nucleotide exchange factor (MyoGEF) at threonine 544 by aurora B kinase promotes the binding of polo-like kinase 1 to MyoGEF.
    Authors: Wu Et al.
    J Biol Chem  2014;289:7142
  20. 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
  21. 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
  22. Oocytes isolated from dairy cows with reduced ovarian reserve have a high frequency of aneuploidy and alterations in the localization of progesterone receptor membrane component 1 and aurora kinase B.
    Authors: Luciano Et al.
    Biol Reprod  2013;88:58
  23. Aurora B spatially regulates EB3 phosphorylation to coordinate daughter cell adhesion with cytokinesis.
    Authors: Ferreira Et al.
    J Cell Biol  2013;201:709
  24. Spatiotemporal organization of Aurora-B by APC/CCdh1 after mitosis coordinates cell spreading through FHOD1.
    Authors: Floyd Et al.
    Cell Cycle  2013;126:2845
  25. In vivo FRET imaging revealed a regulatory role of RanGTP in kinetochore-microtubule attachments via Aurora B kinase.
    Authors: Lee Et al.
    PLoS One  2012;7:e45836
  26. A cell cycle role for the epigenetic factor CTCF-L/BORIS.
    Authors: Rosa-Garrido Et al.
    PLoS One  2012;7:e39371
  27. Haspin inhibitors reveal centromeric functions of Aurora B in chromosome segregation.
    Authors: Wang Et al.
    J Cell Biol  2012;199:251
  28. Appearance and heterochromatin localization of HP1α in early mouse embryos depends on cytoplasmic clock and H3S10 phosphorylation.
    Authors: Meglicki Et al.
    Cell Cycle  2012;11:2189
  29. The chromosomal passenger complex activates Polo kinase at centromeres.
    Authors: Carmena Et al.
    PLoS Biol  2012;10:e1001250
  30. Quantitative phosphoproteomics identifies substrates and functional modules of Aurora and Polo-like kinase activities in mitotic cells.
    Authors: Kettenbach Et al.
    Sci Signal  2011;4:rs5
  31. Aurora kinase B activity is modulated by thyroid hormone during transcriptional activation of pituitary genes.
    Authors: Tardáguila Et al.
    Mol Endocrinol  2011;25:385
  32. 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
  33. 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
  34. Formation of stable attachments between kinetochores and microtubules depends on the B56-PP2A phosphatase.
    Authors: Foley Et al.
    Nat Cell Biol  2011;13:1265
  35. 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
  36. VHL inactivation induces HEF1 and Aurora kinase A.
    Authors: Xu Et al.
    J Cell Biol  2010;21:2041
  37. Relocation of the chromosomal passenger complex prevents mitotic checkpoint engagement at anaphase.
    Authors: Vázquez-Novelle and Petronczki
    Curr Biol  2010;20:1402
  38. Plk1 negatively regulates Cep55 recruitment to the midbody to ensure orderly abscission.
    Authors: Bastos and Barr
    J Cell Biol  2010;191:751
  39. Release of Mps1 from kinetochores is crucial for timely anaphase onset.
    Authors: Jelluma Et al.
    Cell Cycle  2010;191:281
  40. 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
  41. 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
  42. The Aurora kinase inhibitor ZM447439 accelerates first meiosis in mouse oocytes by overriding the spindle assembly checkpoint.
    Authors: Lane Et al.
    Reproduction  2010;140:521
  43. Human condensin function is essential for centromeric chromatin assembly and proper sister kinetochore orientation.
    Authors: Samoshkin Et al.
    PLoS One  2009;4:e6831
  44. 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
  45. 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
  46. Cell cycle dependent degradation of MCAK: evidence against a role in anaphase chromosome movement.
    Authors: Ganguly Et al.
    Toxins (Basel)  2008;7:3187
  47. 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
  48. Cancer cells display profound intra- and interline variation following prolonged exposure to antimitotic drugs.
    Authors: Gascoigne and Taylor
    Cancer Cell  2008;14:111
  49. 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

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