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\u003C0.001)[2]。",{"key":221,"value":222},"体内研究","在GK1X异种移植物系(ns)中,伊马替尼的肿瘤生长抑制百分比(TGI)为83.8％,尼罗替尼为69.6％。在GK2X异种移植物系中,伊马替尼的TGI为83.0％,尼罗替尼(ns)为85.3％。此外,伊马替尼的GK3X异种移植物线TGI为31.1％,尼罗替尼(ns)为47.5％。这些结果表明,除了GK1X异种移植物系外,尼罗替尼显示出与伊马替尼相当或更高的抗肿瘤作用[2]。尼罗替尼对宏观和微观病理评分具有显着的治愈作用,并确保吲哚美辛诱导的小肠结肠炎大鼠模型中相当大的粘膜愈合。虽然尼罗替尼降低了结肠中PDGFRα和β水平以及凋亡评分,但它对体重和TNF-α水平没有显着影响。进一步的实验研究可以为人类提供更明确的证据[3]。",{"key":224,"value":225},"细胞实验","将人GIST细胞系GK1C和GK3C以及伊马替尼抗性细胞系GK1C-IR和GK3C-IR接种于96孔微量培养板中并培养12小时，然后暴露于伊马替尼（1-100μM）或尼罗替尼（1- 100μM）72小时。通过WST-8测定法定量细胞。光密度（OD）由Sunrise rainbow确定。抑制率计算如下：抑制％=（处理组 - 空白的OD）\u002F（对照组 - 空白的OD）×100％。计算导致50％生长抑制的测试药物浓度（IC50）[2]。",{"key":227,"value":228},"动物实验","小鼠[2]使用裸鼠中的GIST异种移植物系GK1X，GK2X和GK3X。通过在BALB \u002F cSLc-nu \u002F nu小鼠中连续传代来维持这些异种移植物系。每天用载体或40mg \u002F kg伊马替尼或尼罗替尼治疗携带GK1X，GK2X和GK3X肿瘤（每组6-8只小鼠）的小鼠，持续4周。根据公式LW2 \u002F 2，根据肿瘤长度（L）和宽度（w）的厚度测量值确定肿瘤体积（TV）。电视每两到三天以及评估当天确定。处死小鼠并且如下计算肿瘤生长抑制（TGI）的百分比：TGI（％）= [1-（评估日的治疗组肿瘤体积 - 治疗组肿瘤体积在第1天的平均值）\u002F（平均值）对照组肿瘤体积对第1天对照组肿瘤体积的评价日均值]]×100。大鼠[3]雌性Wistar白化大鼠，体重226-243g（平均体重，241.09g），用于本研究。以吲哚美辛给药的同一天开始，通过口胃管向Nilotinib组大鼠（n = 7）施用尼罗替尼，以两个分剂量施用20mg \u002F kg \u002F d，持续13天。在13-d期结束时，在乙醚麻醉下从所有大鼠获得用于病理学检查的血液和组织样品。然后通过断头处死所有动物。",{"key":230,"value":231},"参考文献","[1].\nWeisberg E, et al. Beneficial effects of combining nilotinib and imatinib in preclinical models of BCR-ABL+ leukemias. Blood. 2007 Mar 1;109(5):2112-20.\n[2].\nSako H, et al. Antitumor effect of the tyrosine kinase inhibitor Nilotinib on gastrointestinal stromal tumor (GIST) and Imatinib-resistant GIST cells. PLoS One. 2014 Sep 15;9(9):e107613.\n[3].\nDervis Hakim G, et al. Mucosal healing effect of nilotinib in indomethacin-induced enterocolitis: A rat model. 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