PI3K
PI3K (Phosphatidylinositol-4,5-bisphosphate 3-kinase) is a family of enzymes involved in cellular functions such as cell growth, proliferation, differentiation, motility, survival and intracellular trafficking, which in turn are involved in cancer. Many of these functions relate to the ability of class I PI 3-kinases to activate protein kinase B (PKB, aka Akt) as in the PI3K/AKT/mTOR pathway. The p110δ and p110γ isoforms regulate different aspects of immune responses. PI 3-kinases are also a key component of the insulin signaling pathway. The pathway, with oncogene PIK3CA and tumor suppressor PTEN, is implicated in insensitivity of cancer tumors to insulin and IGF1, and in calorie restriction. PI3K family is divided into four different classes: Class I, Class II, Class III, and Class IV. The classifications are based on primary structure, regulation, and in vitro lipid substrate specificity.
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Copanlisib是一个高效的泛I型 PI3K抑制剂，其对PI3Kα/β/γ/δ抑制的IC50分别为0.5, 3.7, 6.4, and 0.7 nM。Phase 3.
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Tersolisib (STX-478) 是一种高效、突变选择性、变构抑制剂 PI3Kα，可选择性靶向 PI3Kα 的常见突变形式。它对常见的 PI3Kα 螺旋和激酶结构域突变（包括 H1047R 变体）具有很强的疗效，IC50 值为 9.4 nmol/L。与野生型相比，STX-478 对突变型 PI3Kα 的选择性高 14 倍。它可以避免代谢功能障碍并改善 PI3Kα 突变异种移植的治疗反应.
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ETP 45658是活性的 PI 3-激酶 抑制剂， 也抑制 DNA-PK，mTOR。
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BAG 956是双效的 PI 3-激酶，PDK1 抑制剂。
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AZD8186是一种特异性的PI3K抑制剂, 有效抑制PI3Kβ (IC50=4 nM) 和PI3Kδ (IC50=12 nM),选择性比PI3Kα (IC50=35 nM) 和PI3Kγ (IC50=675 nM) 高。
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