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JANEX-1迅速消除,消除半衰期为45.6±5.5分钟。虽然预测的最大血浆JANEX-1浓度为10.5±0.8μM,这仅是静脉注射相同推注剂量后Cmax的一半,但ip生物利用度为94.6％且全身暴露水平(即AUC)非常相似静脉注射后观察到的结果(17.1±2.2μM•h对比18.1±1.2μM•h)[3]。",{"key":250,"value":251},"细胞实验","以下细胞系用于各种生物学测定：NALM-6（pre-B-ALL），LC1; 19（pre-B-ALL），DAUDI（B-ALL），RAMOS（B-ALL），MOLT-3 （T细胞ALL），HL60（急性髓性白血病），BT-20（乳腺癌），M24-MET（黑素瘤），SQ20B（鳞状细胞癌）和PC3（前列腺癌）。这些细胞系在培养基中维持。将细胞以50×104细胞\u002F孔的密度接种在6孔组织培养板中，在含有不同浓度的JANEX-1（0.1,0.2,0.3,0.4和0.5nM）的处理培养基中培养24-48小时。在37℃，潮湿的5％CO 2气氛中。使用ApopTag凋亡检测试剂盒[1]通过原位TdT介导的dUTP末端标记试验检测细胞用JANEX-1处理后的细胞凋亡变化。",{"key":253,"value":254},"动物实验","小鼠[2]使用无病原体的8周龄雄性JAK3  -  \u002F  - （129S4-Jak3tm1Ljb）和C57BL \u002F 6J小鼠。在局部缺血前1小时，以20mg \u002F kg（腹膜内）的剂量用JANEX-1处理小鼠。大鼠[3]将雄性Lewis大鼠分成两个实验组，每组5只，并通过阴茎背静脉或腹腔注射单次3.3mg \u002F kg推注剂量的JANEX-1。用甲氧基荧光素麻醉大鼠，静脉注射前或分别在5,10和30分钟以及1,1,5,2,3,4和6小时从大鼠尾静脉采集血样（0.2mL）或在ip注射后5,10,15,30和45分钟以及1,1.5,2,3,4,5和7小时。",{"key":256,"value":257},"参考文献","[1].\nSudbeck EA, et al. Structure-based design of specific inhibitors of Janus kinase 3 as apoptosis-inducing antileukemic agents. Clin Cancer Res. 1999 Jun;5(6):1569-82.\n[2].\nOh YB, et al. Inhibition of Janus activated kinase-3 protects against myocardial ischemia and reperfusion injury in mice. Exp Mol Med. 2013 May 17;45:e23\n[3].\nUckun FM, et al. In vivo toxicity and pharmacokinetic features of the janus kinase 3 inhibitor WHI-P131 [4-(4'hydroxyphenyl)-amino-6,7- dimethoxyquinazoline. Clin Cancer Res. 1999 Oct;5(10):2954-62.\n[4].\nXia F, et al. IL4 (interleukin 4) induces autophagy in B cells leading to exacerbated asthma. 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