An inhibitor of Aurora A kinase activity and the Aurora A-N-Myc protein-protein interaction
CD532 is an inhibitor of Aurora A kinase activity (IC50 = 48 nM) and the protein-protein interaction between N-Myc and Aurora A kinase.1 It also inhibits several cyclin-dependent kinases (CDKs), FGFRs, MEKs, and PDGFRs, as well as FLT3, KIT, and RET at 10 µM.2 CD532 induces degradation of N-Myc in SK-N-BE(2) neuroblastoma cells (EC50 = 223 nM).1 It prevents S-phase entry in SK-N-BE(2) cells when used at a concentration of 1 µM.1 CD532 (25 mg/kg) reduces tumor growth and increases survival in a MYCN-amplified SMS-KCN neuroblastoma mouse xenograft model.
1.Gustafson, W.C., Meyerowitz, J.G., Nekritz, E.A., et al.Drugging MYCN through an allosteric transition in Aurora kinase ACancer Cell26(3)414-427(2014) 2.Lee, J.K., Phillips, J.W., Smith, B.A., et al.N-Myc drives neuroendocrine prostate cancer initiated from human prostate epithelial cellsCancer Cell29(4)536-547(2016)
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