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72小时后，向每个孔中加入10μL55-μM刃天青，并在37℃下孵育4小时。培养后，用荧光光度计测量试卤灵产物，使用560nm的激发波长和590nm的发射波长。使用GraphPad Prism 5软件将IC 50确定为每个平板的阳性和阴性对照组之间的中点。",{"key":249,"value":250},"动物实验","将大鼠随机分配到由载体丙二醇（0.25mL \u002F kg），LY294002（2-（4-吗啉基）-8-苯基-4H-1-苯并吡喃-4-酮组成的药物治疗组;可逆的非特异性PI3K抑制剂; 10 mg \u002F kg），渥曼青霉素（一种不可逆的非特异性PI3K抑制剂; 5 mg \u002F kg），IC87114（2  -  [（6-氨基嘌呤-9-基）甲基] -5-甲基-3-（2 - 甲基苯基）喹唑啉-4-酮;PI3Kp110δ拮抗剂; 2.5mg \u002F kg）和选择性PI3Kp110β拮抗剂TGX221（2.5mg \u002F kg）。在尾部出血实验中，大鼠随机分配到由LY294002（10 mg \u002F kg），IC87114（2.5 mg \u002F kg），渥曼青霉素（5 mg \u002F kg），TGX221（2.5或25 mg \u002F kg）组成的药物治疗组，肝素（100 U \u002F kg），阿司匹林（2×200 mg \u002F kg口服）±肝素（100 U \u002F kg）和阿司匹林（2×200 mg \u002F kg口服）联合肝素（100 U \u002F kg）和TGX221（ 2.5毫克\u002F千克）。除阿司匹林外，所有药物均以0.25 mL \u002F kg的缓慢（超过约45-60 s）静脉推注给予颈静脉。阿司匹林（200mg \u002F kg悬浮在15％阿拉伯树胶水溶液中）口服（口服）两次 - 在实验前24小时给予第一剂量，在实验开始前1小时给予第二剂量。",{"key":252,"value":253},"参考文献","[1].\nZhao Y, et al. Prodrug strategy for PSMA-targeted delivery of TGX-221 to prostate cancer cells. Mol Pharm. 2012 Jun 4;9(6):1705-16.\n[2].\nGe Q, et al. The phosphoinositide 3'-kinase p110δ modulates contractile protein production and IL-6 release in human airway smooth muscle. J Cell Physiol. 2012 Aug;227(8):3044-52.\n[3].\nMüller KM, et al. Role of protein kinase C and epidermal growth factor receptor signalling in growth stimulation by neurotensin in colon carcinoma cells. BMC Cancer. 2011 Oct 2;11:421.\n[4].\nSturgeon SA, et al. Advantages of a selective beta-isoform phosphoinositide 3-kinase antagonist, an anti-thrombotic agent devoid of other cardiovascular actions in the rat. Eur J Pharmacol. 2008 Jun 10;587(1-3):209-15.\n[5].\nChaussade C, et al. Evidence for functional redundancy of class IA PI3K isoforms in insulin signalling. 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