CD532 是一种有效的 Aurora A 激酶抑制剂，IC50 为 45 nM。 CD532 具有阻断 Aurora A 激酶活性和驱动 MYCN 降解的双重作用。 CD532 还可以直接与 AURKA 相互作用并诱导全局构象转变。 CD532可用于癌症的研究。
货号:ajcx24950
CAS:1639009-81-6
分子式:C26H25F3N8O
分子量：522.5
溶解度:Ethanol: soluble
纯度：98%
存储：Store at -20°C
库存：现货

Background:

CD532 is an inhibitor of Aurora A kinase activity (IC₅₀= 48 nM) and the protein-protein interaction between N-Myc and Aurora A kinase.¹It also inhibits several cyclin-dependent kinases (CDKs), FGFRs, MEKs, and PDGFRs, as well as FLT3, KIT, and RET at 10 µM.²CD532 induces degradation of N-Myc in SK-N-BE(2) neuroblastoma cells (EC₅₀= 223 nM).¹It prevents S-phase entry in SK-N-BE(2) cells when used at a concentration of 1 µM.¹CD532 (25 mg/kg) reduces tumor growth and increases survival in aMYCN-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)