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ZM 447439, 5 mg  

ZM 447439, 5 mg

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

Synonyms: ZM447439, ZM-447439
selective ATP-competitive inhibitor of Aurora B kinase

More details

PKI-ZM447-005

Availability: within 3 days

195,00 €

Background: ZM 447439 is a 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). It is selective over a range of other kinases including cdk1 and PLK1 (IC50 > 10 µM) and inhibits cell division, mitotic phosphorylation of histone H3, a physiologically relevant target of Aurora B, and caused defects in chromosome alignment, chromosome segregation and cytokinesis, most likely by interfering with the spindle integrity. ZM 447439 displays selective toxicity towards proliferating tumour cells versus non-dividing cells.

Chemical formula: C29H31N5O4 x 3H20
Molecular Weight:  587,71 g/mol
Purity:  >99%
Appearance:  cristalline, off white solid
Solubility:  soluble in DMSO (0,1 M), freely soluble in acetic acid, soluble in toluene, slightly soluble in acetonitrile
CAS number: 331771-20-1

Product specific literature references:

Girdler F, Gascoigne KE, Eyers PA, Hartmuth S, Crafter C, Foote KM, Keen NJ, Taylor SS. (2006) " Validating Aurora B as an anti-cancer drug target." J Cell Sci.;119(Pt 17):3664-75.

Ditchfield C, Keen N, Taylor SS. (2005) " The Ipl1/Aurora kinase family: methods of inhibition and functional analysis in mammalian cells." Methods Mol Biol. 296:371-81.

Ditchfield C, Johnson VL, Tighe A, Ellston R, Haworth C, Johnson T, Mortlock A, Keen N, Taylor SS. (2003) " Aurora B couples chromosome alignment with anaphase by targeting BubR1, Mad2, and Cenp-E to kinetochores." J Cell Biol. 161(2):267-80.

Doggrell SA. (2004) "Dawn of Aurora kinase inhibitors as anticancer drugs." Expert Opin Investig Drugs. 13(9):1199-201.

Gadea BB, Ruderman JV. (2005) �Aurora kinase inhibitor ZM447439 blocks chromosome-induced spindle assembly, the completion of chromosome condensation, and the establishment of the spindle integrity checkpoint in Xenopus egg extracts." Mol Biol Cell.16(3):1305-18.