2. Academic Validation
  3. Synthesis and Evaluation of Novel C-X-C Chemokine Receptor 4-Targeted Radiotracers for Oncological Imaging

Synthesis and Evaluation of Novel C-X-C Chemokine Receptor 4-Targeted Radiotracers for Oncological Imaging

  • J Med Chem. 2025 Aug 28;68(16):17221-17235. doi: 10.1021/acs.jmedchem.5c00735.
Yanzhi Wang 1,  Jingyue Gao 1,  Yuze Ma 1,  Yuan Pan 1,  Kunyao Wang 1,  Wenqi Zhao 1,  Feng Gao 1
Affiliations

Affiliation

  • 1 Key Laboratory for Experimental Teratology of the Ministry of Education and Center for Experimental Nuclear Medicine, School of Basic Medical Sciences, Cheeloo College of Medicine, Shandong University, Jinan, Shandong 250012, China.
PMID: 40828001 DOI: 10.1021/acs.jmedchem.5c00735
Abstract

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 high radiochemical purity (>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.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-175882
    CXCR4 ligand