ZM 447439

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Cat.No. 2458 - ZM 447439 | C29H31N5O4 | CAS No. 331771-20-1
Description: Inhibits Aurora kinase B
Chemical Name: N-[4-[[6-Methoxy-7-[3-(4-morpholinyl)propoxy]-4-quinazolinyl]amino]phenyl]benzamide
Purity: ≥98% (HPLC)
Datasheet
Citations (25)
Literature

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.

Licensing Information

Sold with the permission of AstraZeneca UK Ltd.

Compound Libraries

ZM 447439 is also offered as part of the Tocriscreen Plus, Tocriscreen Kinase Inhibitor Toolbox I and Tocriscreen Epigenetics Toolbox. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 513.59
Formula C29H31N5O4
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 331771-20-1
PubChem ID 9914412
InChI Key OGNYUTNQZVRGMN-UHFFFAOYSA-N
Smiles COC1=CC2=C(NC3=CC=C(NC(=O)C4=CC=CC=C4)C=C3)N=CN=C2C=C1OCCCN1CCOCC1

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 51.36 100

Preparing Stock Solutions

The following data is based on the product molecular weight 513.59. 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 1.95 mL 9.74 mL 19.47 mL
5 mM 0.39 mL 1.95 mL 3.89 mL
10 mM 0.19 mL 0.97 mL 1.95 mL
50 mM 0.04 mL 0.19 mL 0.39 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.

Ditchfield et al (2003) Aurora B couples chromosome alignment with anaphase by targeting BubR1, Mad2, and Cenp-E to kinetochores. J.Cell Biol. 161 267 PMID: 12719470

Jung et al (2006) Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors. J.Med.Chem. 49 955 PMID: 16451062

Girdler et al (2006) Validating Aurora B as an anti-cancer drug target. J.Cell Sci. 119 3664 PMID: 16912073


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Keywords: ZM 447439, supplier, inhibitors, inhibits, Aurora, kinases, B, Mitosis, ZM447439, AstraZeneca, Aurora, Kinases, Tocris Bioscience

25 Citations for ZM 447439

Citations are publications that use Tocris products. Selected citations for ZM 447439 include:

Kasuboski et al (2011) Zwint-1 is a novel Aurora B substrate required for the assembly of a dynein-binding platform on kinetochores. Mol Biol Cell 22 3318 PMID: 21775627

Tardáguila et al (2011) Aurora kinase B activity is modulated by thyroid hormone during transcriptional activation of pituitary genes. Mol Endocrinol 25 385 PMID: 21239609

Yuan et al (2011) Polo-box domain inhibitor poloxin activates the spindle assembly checkpoint and inhibits tumor growth in vivo. Am J Pathol 179 2091 PMID: 21839059

Foley et al (2011) Formation of stable attachments between kinetochores and microtubules depends on the B56-PP2A phosphatase. Nat Cell Biol 13 1265 PMID: 21874008

Vázquez-Novelle and Petronczki (2010) Relocation of the chromosomal passenger complex prevents mitotic checkpoint engagement at anaphase. Curr Biol 20 1402 PMID: 20619651

Manchado et al (2010) Targeting mitotic exit leads to tumor regression in vivo: Modulation by Cdk1, Mastl, and the PP2A/B55α,δ phosphatase. Cancer Cell 18 641 PMID: 21156286

Bastos and Barr (2010) Plk1 negatively regulates Cep55 recruitment to the midbody to ensure orderly abscission. J Cell Biol 191 751 PMID: 21079244

Pal et al (2010) Role of a novel coiled-coil domain-containing protein CCDC69 in regulating central spindle assembly. J Am Soc Nephrol 9 4117 PMID: 20962590

Xu et al (2010) VHL inactivation induces HEF1 and Aurora kinase A. J Cell Biol 21 2041 PMID: 20864688

Jelluma et al (2010) Release of Mps1 from kinetochores is crucial for timely anaphase onset. Cell Cycle 191 281 PMID: 20937696

Bassett et al (2010) Epigenetic centromere specification directs aurora B accumulation but is insufficient to efficiently correct mitotic errors. Mol Cancer Ther 190 177 PMID: 20643881

Scutt et al (2009) Discovery and exploitation of inhibitor-resistant aurora and polo kinase mutants for the analysis of mitotic networks. J Biol Chem 284 15880 PMID: 19359241

Platani et al (2009) The Nup107-160 nucleoporin complex promotes mitotic events via control of the localization state of the chromosome passenger complex. Mol Biol Cell 20 5260 PMID: 19864462

Samoshkin et al (2009) Human condensin function is essential for centromeric chromatin assembly and proper sister kinetochore orientation. PLoS One 4 e6831 PMID: 19714251

Slawson et al (2008) A mitotic GlcNAcylation/phosphorylation signaling complex alters the posttranslational state of the cytoskeletal protein vimentin. Mol Biol Cell 19 4130 PMID: 18653473

Ganguly et al (2008) Cell cycle dependent degradation of MCAK: evidence against a role in anaphase chromosome movement. Toxins (Basel) 7 3187 PMID: 18843200

Vischioni et al (2006) Frequent overexpression of aurora B kinase, a novel drug target, in non-small cell lung carcinoma patients. Mol Cancer Ther 5 2905 PMID: 17121938

Kim and Yu (2015) Multiple assembly mechanisms anchor the KMN spindle checkpoint platform at human mitotic kinetochores. J Cell Biol 208 181 PMID: 25601404

Platani et al (2015) Mio depletion links mTOR regulation to Aurora A and Plk1 activation at mitotic centrosomes. J Cell Biol 210 45 PMID: 26124292

Tauchman et al (2015) Stable kinetochore-microtubule attachment is sufficient to silence the spindle assembly checkpoint in human cells. J Cell Sci 6 10036 PMID: 26620470

Balboula and Schindler (2014) Selective disruption of aurora C kinase reveals distinct functions from aurora B kinase during meiosis in mouse oocytes. PLoS Genet 10 e1004194 PMID: 24586209

Mäki-Jouppila et al (2014) Centmitor-1, a novel acridinyl-acetohydrazide, possesses similar molecular interaction field and antimitotic cellular phenotype as rigosertib, on 01910.Na. Nat Commun 13 1054 PMID: 24748653

Ferreira et al (2013) Aurora B spatially regulates EB3 phosphorylation to coordinate daughter cell adhesion with cytokinesis. J Cell Biol 201 709 PMID: 23712260

Floyd et al (2013) Spatiotemporal organization of Aurora-B by APC/CCdh1 after mitosis coordinates cell spreading through FHOD1. Cell Cycle 126 2845 PMID: 23613471

Wang et al (2012) Haspin inhibitors reveal centromeric functions of Aurora B in chromosome segregation. J Cell Biol 199 251 PMID: 23071152


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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.

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