11C-AZD9291 分子探针检测肺癌EGFR 19del 突变的实验研究

目的 从动物实验探索11C-AZD9291 作为PET/CT 示踪剂检测肺癌EGFR 19del 突变的可行性。 方法 将普通昆明小鼠随机分组并尾静脉注射11C-AZD9291，分别于不同时间点取不同小鼠器官并计算放射 性摄取率。选取EGFR 19del 突变的HCC827、EGFR 野生型A549 肺腺癌细胞株并复制肺癌裸鼠模型，挑选 合格的HCC827 荷瘤鼠6 只分为实验组和阻断组。实验组尾静脉注射11C-AZD9291 ；阻断组同时注射阻断 剂厄洛替尼标准品和11C-AZD9291，另取3 只A549 荷瘤鼠仅尾静脉注射11C-AZD9291 作为对照组，20 min 后行micro-PET 动物活体显像与分析。结果 普通昆明小鼠中11C-AZD9291 在肝脏中放射性摄取率最高， 其次为肾脏、肺，5 min 时血、肝、肾、肺、心及肌肉放射性摄取率较15 min 时高（P <0.05）。实验组标准 摄取值高于对照组和阻断组（P <0.05）。结论 11C-AZD9291 是一种可行的检测肺癌EGFR 19del 突变的分 子探针。

Experimental study on the detection of EGFR 19del mutation in lung cancer by 11C-AZD9291 molecular probe

Objective To explore the feasibility of 11C-AZD9291 as a Micro PET-CT tracer for the detection of EGFR 19del mutation in lung cancer at the level of experimental animals. Methods The normal Kunming mice were injected with 11C-AZD9291 via tail vein, and were executed at different time points. The radioactive counting (%ID/g) was calculated for multiple organs of the mice. Lung adenocarcinoma cell lines HCC827 (EGFR 19del mutation) and A549 (EGFR wild-type) were used to construct the nude mouse models of lung cancer. Six eligible nude mice with HCC827 tumor were selected, and were divided into experimental group and blocking group. In the experimental group, 11C-AZD9291 was injected into the tail vein. The blocking group was injected with erlotinib and 11C-AZD9291 simultaneously. Other three nude mice transplanted with A549 was injected 11C-AZD9291 via tail vein as EGFR wildtype control group. After 20min, animal in-vivo imaging and analysis were performed by micro-pet (Explore Vista, GE). The independent-samples T test and one way ANOVA were used for statistical analysis. Results Kunming mice had the highest radiation uptake rate of 11C-AZD9291 in the liver, followed by kidney and lung. The radiation uptake rate in each organ at time point of 5min was higher than that at 15min (P < 0.05). And the radiation uptake rate in experiment group was higher than that in blocking group or control group. Conclusions At the level of experimental animals, 11C-AZD9291 is a good specific molecular probe for the detection of EGFR 19del mutation in lung cancer.