At present, the early diagnosis and treatment of NSCLC has become an international research hotspot. However, how to realize the organic combination of highly sensitive and high-resolution tumor imaging diagnosis and effective treatment, and to provide effective information for the diagnosis and treatment of cancer is still a major problem in the integration of cancer diagnosis and treatment. In this study, based on the Crizotinib has a good targeted inhibitory effect on ALK positive tumor cells, the near-infrared targeted fluorescent dye IR-780 was covalently bound with the drug molecule Crizotinib, thus the near-infrared fluorescent probe IR-780-Crizotinib targeting ALK positive tumor cells was synthesized. The probe structure is confirmed by NMR and MS. The optical properties of the fluorescent probe and the imaging process in ALK positive tumor-bearing mice were analyzed using ultraviolet spectrophotometer, near-infrared fluorescence spectrometer, and near-infrared fluorescence imaging system. The results show that the probe had better photoactivity. In vivo imaging shows that the probe maintained the biological activity of Crizotinib, effectively targeting the tumor site involved with clear imaging, and ultimately excreted from the body. It was confirmed that the probe could be used for the tracking, positioning and targeted therapy of nude mice with ALK positive tumors in vivo, thus exploring a new approach for the clinical application of near-infrared fluorescent probe to detect ALK positive tumors in the future.

目前，NSCLC的早期诊断和治疗已成为国际研究热点。然而，如何实现高灵敏度、高分辨率的肿瘤影像诊断与有效治疗的有机结合，为肿瘤的诊疗提供有效的信息，仍是肿瘤诊疗一体化的一大难题。本研究基于克唑替尼对ALK阳性肿瘤细胞具有良好的靶向抑制作用，将近红外靶向荧光染料IR-780与药物分子克唑替尼共价结合，从而制备出近红外荧光探针IR-780-合成了靶向 ALK 阳性肿瘤细胞的克唑替尼。探针结构通过NMR和MS确认。使用紫外分光光度计、近红外荧光光谱仪和近红外荧光成像系统分析了荧光探针的光学特性和ALK阳性荷瘤小鼠的成像过程。结果表明该探针具有较好的光活性。体内成像显示，该探针保持了克唑替尼的生物学活性，有效靶向肿瘤部位，成像清晰，最终排出体外。证实该探针可用于体内ALK阳性肿瘤裸鼠的跟踪、定位和靶向治疗，为未来临床应用近红外荧光探针检测ALK阳性肿瘤探索新途径. 近红外荧光光谱仪和近红外荧光成像系统。结果表明该探针具有较好的光活性。体内成像显示，该探针保持了克唑替尼的生物学活性，有效靶向肿瘤部位，成像清晰，最终排出体外。证实该探针可用于体内ALK阳性肿瘤裸鼠的跟踪、定位和靶向治疗，为未来临床应用近红外荧光探针检测ALK阳性肿瘤探索新途径. 近红外荧光光谱仪和近红外荧光成像系统。结果表明该探针具有较好的光活性。体内成像显示，该探针保持了克唑替尼的生物学活性，有效靶向肿瘤部位，成像清晰，最终排出体外。证实该探针可用于体内ALK阳性肿瘤裸鼠的跟踪、定位和靶向治疗，为未来临床应用近红外荧光探针检测ALK阳性肿瘤探索新途径. 有效靶向肿瘤部位，清晰成像，最终排出体外。证实该探针可用于体内ALK阳性肿瘤裸鼠的跟踪、定位和靶向治疗，为未来临床应用近红外荧光探针检测ALK阳性肿瘤探索新途径. 有效靶向肿瘤部位，清晰成像，最终排出体外。证实该探针可用于体内ALK阳性肿瘤裸鼠的跟踪、定位和靶向治疗，为未来临床应用近红外荧光探针检测ALK阳性肿瘤探索新途径.