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Biological Activity:
Selective and ATP-competitive inhibitor of Aurora B kinase in vitro, with IC50 values to be 50, 250 and 1000 nM for Aurora B, C and A kinases respectively.
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 in xenopus egg extracts. Mol. Biol. Cell 2005, 16(3), 1305-1318. [online]
AA Dar et al. Aurora Kinase Inhibitors - Rising Stars in Cancer Therapeutics?
Mol. Cancer Ther. 2010, 9(2), 268 - 278. [online]
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 in gastroenteropancreatic neuroendocrine tumor cell lines. Neuroendocrinol. 2010, 91(2), 121-130.
Chemical Name: N-[4-[[6-Methoxy-7-[3-(4-morpholinyl)propoxy]-4-quinazo linyl]amino]phenyl]benzamide
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