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ZM 447439
- Soluble in DMSO
- MF: C29H31N5O4
- MW: 513.59
Description
ZM 447439 is a selective, ATP-competitive Aurora kinase inhibitor with strongest activity against Aurora B, exhibiting IC50 values of 50, 250 and 1000 nM for Aurora B, C and A kinases respectively.
Aurora B controls chromosome alignment, spindle checkpoint signaling and cytokinesis as part of the chromosomal passenger complex. ZM 447439 is a standard tool for studying Aurora B-dependent mitotic events, polyploidy and cell-cycle failure.
Key Features
- ATP-competitive Aurora kinase inhibitor
- Preferential activity against Aurora B over Aurora A
- Disrupts chromosome segregation and cytokinesis
- Established tool for mitotic checkpoint research
Applications
- Aurora B kinase assays
- Chromosomal passenger complex studies
- Mitosis and cytokinesis research
- Cell-cycle arrest and polyploidy models
More Information
| Parent CAS No. | 331771-20-1 |
|---|---|
| Chemical Name | N-{4-[6-Methoxy-7-(3-morpholin-4-yl-propoxy)-quinazolin-4-ylamino]-phenyl}-benzamide |
| SMILES | C1(OCCCN2CCOCC2)C=C2N=CN=C(NC3C=CC(NC(C4C=CC=CC=4)=O)=CC=3)C2=CC=1OC |
| MFCD | MFCD08703125 |
| InChi | InChI=1S/C29H31N5O4/c1-36-26-18-24-25(19-27(26)38-15-5-12-34-13-16-37-17-14-34)30-20-31-28(24)32-22-8-10-23(11-9-22)33-29(35)21-6-3-2-4-7-21/h2-4,6-11,18-20H,5,12-17H2,1H3,(H,33,35)(H,30,31,32) |
| InChiKey | OGNYUTNQZVRGMN-UHFFFAOYSA-N |
| CID | 9914412 |
| Short Description | Aurora B inhibitor |
References
- BB Gadea and JV Ruderman. Aurora kinase inhibitor ZM447439 blocks chromosome-induced spindle assembly, the completion of chromosome condensation, and the establishment of the spindle integrity checkpoint. Mol. Biol. Cell 2005, 16(3), 1305-1318.
- AA Dar et al. Aurora Kinase Inhibitors - Rising Stars in Cancer Therapeutics? Mol. Cancer Ther. 2010, 9(2), 268 - 278.
- F Girdler et al. Validating Aurora B as an anti-cancer drug target. J. Cell. Sci. 2006, 119, 3664-75.
- C Ditchfield et al. Aurora B couples chromosome alignment with anaphase by targeting BubR1, Mad2, and Cenp-E to kinetochores. J. Cell. Biol. 2003, 161(2), 267-80.
- I Georgieva et al. ZM447439, A novel promising aurora kinase inhibitor, Provokes antiproliferative and proapoptotic effects alone and in combination with Bio- and chemotherapeutic agents... Neuroendocrinol. 2010, 91(2), 121-130.
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