| 1440085-05-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• CAS: 1440085-05-1
• 化学式: C₂₇H₂₆BNO₃
• 分子量: 423.319
• InChiKey: XOHKKUVIOUMRMX-UHFFFAOYSA-N

反应信息

• 作为反应物：
  描述：

  、 在 (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride 、 potassium carbonate 作用下， 以 乙二醇二甲醚 、 水 为溶剂， 生成 3-[3-(4-Methylpiperazin-1-yl)cyclobutyl]-1-(4-phenoxy-2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-8-amine
  参考文献：
  名称：

  Discovery of Novel Insulin-Like Growth Factor-1 Receptor Inhibitors with Unique Time-Dependent Binding Kinetics

  摘要：

  This letter describes a series of small molecule inhibitors of IGF-1R with unique time-dependent binding kinetics and slow off-rates. Structure activity and structure kinetic relationships were elucidated and guided further optimizations within the series, culminating in compound 2. With an IGF-1R dissociative half-life (t(1/2)) of >100 h, compound 2 demonstrated, significant and extended pp effects in conjunction with tumor growth inhibition to xenograft models at a remarkably low and intermittent dose, which correlated with the observed in vitro slow off-rate properties.

  DOI：

  10.1021/ml400160a