2. Academic Validation
  3. 18F-Radiolabeling and Evaluation of an AMD3465 Derivative for PET Imaging of CXCR4 in a Mouse Breast Tumor Model

18F-Radiolabeling and Evaluation of an AMD3465 Derivative for PET Imaging of CXCR4 in a Mouse Breast Tumor Model

  • Bioconjug Chem. 2024 May 15;35(5):567-574. doi: 10.1021/acs.bioconjchem.4c00167.
Huiqiang Li 1 2,  Xiaochen Li 2,  Lingyi Sun 3,  Yanjie He 1,  Li Wang 4,  Yongju Gao 2,  Dexing Zeng 3,  Xinchang Pang 1,  Junling Xu 2
Affiliations

Affiliations

  • 1 Henan Joint International Research Laboratory of Living Polymerizations and Functional Nanomaterials, Henan Key Laboratory of Advanced Nylon Materials and Application, School of Materials Science and Engineering, Zhengzhou University, Zhengzhou 450001, China.
  • 2 Department of Nuclear Medicine, Henan Key Laboratory of Novel Molecular Probes and Clinical Translation in Nuclear Medicine, Henan Provincial People's Hospital & the People's Hospital of Zhengzhou University, Zhengzhou 450003, China.
  • 3 Molecular Imaging Laboratory, Department of Medicine, University of Pittsburgh, 3501 Fifth Avenue, Pittsburgh, Pennsylvania 15261, United States.
  • 4 Henan Academy of Medical Sciences, Zhengzhou 450003, China.
PMID: 38634516 DOI: 10.1021/acs.bioconjchem.4c00167
Abstract

The exploration of pharmaceutically active agents and positron emission tomography (PET) tracers targeting CXCR4 has been a focal point in Cancer research given its pivotal role in the development and progression of various cancers. While significant strides have been made in PET imaging with radiometal-labeled tracers, the landscape of 18F-labeled small molecule tracers remains relatively limited. Herein, we introduce a novel and promising derivative, [18F]SFB-AMD3465, as a targeted PET tracer for CXCR4. The compound was synthesized by modifying the pyridine ring of AMD3465, which was subsequently labeled with 18F using [18F]SFB. The study provides comprehensive insights into the design, synthesis, and biological evaluation of [18F]SFB-AMD3465. In vitro and in vivo assessments demonstrated the CXCR4-dependent, specific, and sensitive uptake of [18F]SFB-AMD3465 in the CXCR4-overexpressing 4T1 cell line and the corresponding xenograft-bearing mouse model. These findings contribute to bridging the gap in 18F-labeled PET tracers for CXCR4 and underscore the potential of [18F]SFB-AMD3465 as a PET radiotracer for in vivo CXCR4 imaging.

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