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C-X-C chemokine receptor-4 (CXCR4), which is overexpressed in various cancers, has been considered as an important target for cancer theranostics. In this study, a series of small molecule radiotracers targeting CXCR4 were developed and obtained with radiochemical purity over 95%. Among seven radiotracers, [68Ga]Ga-SDNUM04 showed favorable binding affinity (Kd: 32.21 ± 0.71 nM), tumor uptake (SUVmean: 0.63 ± 0.02) and tumor-to-liver ratio (T/L: 1.07). In addition, [68Ga]Ga-SDNUM04 exhibited satisfactory imaging outcomes and biodistribution properties in various CXCR4-positive tumors, making it a promising radiotracer for the clinical diagnosis of CXCR4-positive cancers.

C-X-C趋化因子受体4（CXCR4）在多种癌症中高表达，被视为癌症诊疗一体化（theranostics）的重要靶点。本研究开发了一系列靶向CXCR4的小分子放射性示踪剂（radiotracers），其放射化学纯度均超过95%。在七种示踪剂中，[68Ga]Ga-SDNUM04表现出良好的结合亲和力（binding affinity）（Kd：32.21±0.71 nM）、肿瘤摄取率（tumor uptake）（SUVmean：0.63±0.02）及肿瘤-肝脏比值（tumor-to-liver ratio）（T/L：1.07）。此外，[68Ga]Ga-SDNUM04在多种CXCR4阳性肿瘤中展现出理想的成像效果（imaging outcomes）及生物分布特性（biodistribution properties），使其成为CXCR4阳性癌症临床诊断的潜在候选示踪剂。