磷脂酰肌醇-3-激酶(PI3K)是一类重要的细胞信号传导分子,可调节细胞的生长、代谢、增殖以及血管生成,在许多肿瘤组织中被异常激活,其信号通路如PI3K/mTOR(哺乳动物雷帕霉素靶蛋白)/Akt通路,在肿瘤发生发展中起重要作用,其中ⅠA类PI3K与肿瘤的关系最为密切,也已成为肿瘤治疗的重要靶标。早期的Ⅰ类PI3K抑制剂如渥曼青霉素,虽具有体内抗肿瘤活性,但因溶解性、药动 Phosphatidylinositol 3-kinase (PI3K) is an important class of cell signaling molecules that regulate cell growth, metabolism, proliferation and angiogenesis and is abnormally activated in many tumor tissues. Its signaling pathway, such as PI3K / mTOR (Mammalian target of rapamycin) / Akt pathway plays an important role in the development of tumors. Class IA PI3K has the closest relationship with tumor and has become an important target of tumor therapy. Early class PI3K inhibitors such as wortmannin, although with in vivo antitumor activity, but due to solubility, pharmacokinetics