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nM。",{"key":229,"value":230},"相关类别","信号通路\n>>\n自噬\n>>\n自噬\n信号通路\n>>\n蛋白酪氨酸激酶\n>>\nBCR-ABL\n信号通路\n>>\n蛋白酪氨酸激酶\n>>\nSRC\n研究领域\n>>\n癌症",{"key":232,"value":233},"靶点","IC50: 0.6 nM\u002F0.8 nM (AblWT\u002FSrc)[1] IC50: 79 nM\u002F37 nM (c-KitWT\u002Fc-KitD816V)[2]",{"key":235,"value":236},"体外研究","达沙替尼在较窄的范围内(IC50≤1.7nM)有效抑制野生型Abl激酶和除T315I外的所有突变体。与伊马替尼相比,达沙替尼(IC50：0.8 nM)对Ba\u002FF3细胞中表达野生型Bcr-Abl的细胞的效力高出325倍[1]。",{"key":238,"value":239},"体内研究","在第10天开始每日用达沙替尼(50mg\u002Fkg)治疗。使用该方法,在治疗后6天(第16天,P = 0.014)观察到BCPAP原位肿瘤生长的显着抑制,其持续至第23天和与载体治疗的小鼠相比,29(P = 0.0003)[3]。达沙替尼(50 mg\u002Fkg)在大鼠中的代谢研究表明,达沙替尼是主要的循环成分,而多种代谢物在给药后4小时对剩余的40-60％的样品放射性有贡献[4]。",{"key":241,"value":242},"激酶实验","使用野生型和突变型谷胱甘肽S-转移酶（GST）-Ab1融合蛋白（c-Abl氨基酸220-498）的激酶测定进行了微小的改变。 GST-Abl融合蛋白在使用前从谷胱甘肽 - 琼脂糖珠中释放出来; ATP的浓度为5μM。在用于激酶自身磷酸化和体外肽底物磷酸化测定之前，立即用LAR酪氨酸磷酸酶处理GST-Abl激酶结构域融合蛋白。在30℃温育1小时后，通过加入钒酸钠（1mM）使LAR磷酸酶失活。使用磷酸酪氨酸特异性抗体4G10常规地进行比较未处理的GST-Abl激酶与去磷酸化的GST-Abl激酶的免疫印迹分析以确认酪氨酸残基和c-Abl抗体CST 2862的完全（> 95％）去磷酸化以确认GST-Abl的相等加载。激酶。 IC50测定的抑制剂浓度范围是0至5,000nM（伊马替尼和AMN107）或0至32nM（达沙替尼）。对于突变体T315I，达沙替尼浓度范围扩展至1,000nM。这些相同的抑制剂浓度用于体外肽底物磷酸化测定。在针对GST-Src激酶和GST-Lyn激酶的这些相同浓度范围内测试三种抑制剂。",{"key":244,"value":245},"细胞实验","将Ba \u002F F3细胞系一式三份接种，并与升高浓度的伊马替尼，AMN107或达沙替尼一起孵育72小时。使用基于甲硫基磺酸盐的活力测定（CellTiter96 Aqueous One Solution Reagent）测量增殖。 IC50和IC90值报告为一式四份进行的三次独立实验的平均值。 IC50和IC90测定的抑制剂浓度范围为0至2,000nM（伊马替尼和AMN107）或0至32nM（达沙替尼）。对于IC 50> 2,000 nM的突变体，伊马替尼浓度范围扩展至6,400 nM。对于突变体T315I，达沙替尼浓度范围扩展至200nM。",{"key":247,"value":248},"动物实验","小鼠[3]使用雄性无胸腺裸鼠（25克; 5周龄）。制备达沙替尼（50mg \u002F kg）用于在pH 3.0的80mM柠檬酸钠缓冲液中每日口服强饲（5天\u002F周）。对于原位鼠模型，在第10天基于生物发光活性将小鼠随机化以接受药物或媒介物。在转移性小鼠模型中，小鼠接受达沙替尼或载体，如前所述，在心内注射（预处理）之前2天开始，或在随机化（治疗后）后第11天开始。大鼠[4]达沙替尼以0.5mg \u002F kg口服0.5％甲基纤维素给予雄性Wistar-Han（WH）大鼠。自动化大鼠血液采集装置被编程为以预定间隔收集200μL血液。在每个时间点，将accusampler编程为将20μL血液直接发现两次（两个点）到DBS卡上。将剩余的160μL液体血液收集到含EDTA钠的管中。在以11,000rpm立即离心血液5分钟后获得血浆样品。将血浆样品储存在-80℃直至分析。将DBS样品在室温下干燥至少2小时并储存在干燥器中的塑料袋中直至样品分析。",{"key":250,"value":251},"参考文献","[1].\nO'Hare T, et al. In vitro activity of Bcr-Abl inhibitors AMN107 and BMS-354825 against clinically relevant imatinib-resistant Abl kinase domain mutants. Cancer Res. 2005 Jun 1;65(11):4500-5.\n[2].\nShah NP, et al. Dasatinib (BMS-354825) inhibits KITD816V, an imatinib-resistant activating mutation that triggers neoplastic growth in most patients with systemic mastocytosis. Blood. 2006 Jul 1;108(1):286-91.\n[3].\nChan CM, et al. Targeted inhibition of Src kinase with dasatinib blocks thyroid cancer growth and metastasis. Clin Cancer Res. 2012 Jul 1;18(13):3580-91.\n[4].\nShen Z, et al. Metabolite profiling of dasatinib dosed to Wistar Han rats using automated dried blood spot collection. J Pharm Biomed Anal. 2012 Aug-Sep;67-68:92-7.\n[5].\nWeisberg E, et al. Using combination therapy to override stromal-mediated chemoresistance in mutant FLT3-positive AML: synergism between FLT3 inhibitors, dasatinib\u002Fmulti-targeted inhibitors and JAK inhibitors. Leukemia. 2012 Oct;26(10):2233-44.\n[6].\nKan He, et al. Protein kinase inhibitors. Patent. 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