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kg的低剂量下表现出剂量依赖性肿瘤生长抑制。此外,Omipalisib(GSK2126458)在四种临床前物种(小鼠,大鼠,狗和猴子)中显示出低血液清除率和良好的口服生物利用度[1]。",{"key":248,"value":249},"细胞实验","将BT474，HCC1954和T-47D（人乳房）在含有10％胎牛血清的RPMI-1640中于37℃在5％CO 2培养箱中培养。在测定设定密度之前，将细胞分成T75培养瓶2至3天，在收获时产生约70-80％的汇合用于测定。使用0.25％胰蛋白酶-EDTA收获细胞。使用台盼蓝排除染色对细胞悬浮液进行细胞计数。然后将细胞以每孔1,000个细胞接种于384孔黑色平底聚苯乙烯中，每孔48μL培养基中。将所有平板置于5％CO 2,37℃过夜，第二天加入Omipalisib（GSK2126458）。将一个平板用CellTiter-Glo处理第0天（t = 0）测量并如下所述读取。 Omipalisib（GSK2126458）在透明底部聚丙烯384孔板中制备，连续两倍稀释。将4μL这些稀释液加入到105μL培养基中，混合溶液后，将2μL这些稀释液加入细胞板的每个孔中。所有孔中DMSO的最终浓度为0.15％。将细胞在37℃，5％CO 2下孵育72小时。用Omipalisib孵育72小时后，开发并读取每个平板。使用等于孔中细胞培养物体积的体积将CellTiter-Glo试剂添加至测定板。将板振荡约2分钟并在室温下孵育约30分钟，并在Analyst GT读数器上读取化学发光信号。结果表示为t = 0的百分比，并相对于Omipalisib（GSK2126458）浓度作图。通过使用XLfit软件拟合4或6参数曲线拟合的剂量响应并确定抑制50％细胞生长（gIC50）的浓度，以Y min作为t = 0，确定Omipalisib（GSK2126458）的细胞生长抑制。和Y max作为DMSO对照。从所有样品中减去没有细胞的孔的值用于背景校正。",{"key":251,"value":252},"参考文献","[1].\nKnight SD, et al. 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