693228-63-6

CYC116 is a potent inhibitor of Aurora A/B and VEGFR with Ki of 8.0 nM/9.2 nM and 44 nM, respectively.

CYC116 is an orally active small molecule multi-kinase inhibitor with anti-neoplastic activity. CYC116 inhibits Aurora kinases A/B and vascular endothelial growth factor receptor 2 (VEGFR2), resulting in disruption of the cell cycle, rapid cell death, and the inhibition of angiogenesis.

the anticancer effects of cyc116 were shown to emanate from cell death following mitotic failure and increased polyploidy as a consequence of cellular inhibition of aurora a and b kinases. moreover, cyc116 was also assessed against other kinases [1].

preliminary in vivo assessment showed that cyc116 was orally bioavailable and possessed anticancer activity. the mean relative tumor volumes of mice receiving cyc116 at both dose levels were less than those of vehicle-treated mice for the duration of the study period [1].

Aurora A

44 and 19 nm respectively for aurora a and b in cancer cells

Store at -20°C

[1] wang s, midgley ca, sca?rou f, grabarek jb, griffiths g, jackson w, kontopidis g, mcclue sj, mcinnes c, meades c, mezna m, plater a, stuart i, thomas mp, wood g, clarke rg, blake dg, zheleva di, lane dp, jackson rc, glover dm, fischer pm. discovery of n-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors. j med chem. 2010;53(11):4367-78.