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Updated: Feb 15, 2026

Preparation and Evaluation of 99mTc-labeled Tridentate Chelates for Pre-targeting Using Bioorthogonal Chemistry
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Development of a novel 99m Tc-labeled small molecular antagonist for CXCR4 positive tumor imaging

Xuran Zhang1,2, Linyi You3, Shuting Chen1

  • 1Key Laboratory of Radiopharmaceuticals (Beijing Normal University), Ministry of Education; College of Chemistry, Beijing Normal University, Beijing, PR China.

Journal of Labelled Compounds & Radiopharmaceuticals
|January 26, 2018
PubMed

Insights

Technetium-99m-labeled AMD3465 effectively targets chemokine receptor 4 (CXCR4) in preclinical models. This radiotracer shows promise for imaging CXCR4-positive tumors using single photon emission computed tomography.

Area of Science:

  • Oncology
  • Radiochemistry
  • Molecular Imaging

Background:

  • Chemokine receptor 4 (CXCR4) is overexpressed in numerous cancers, driving tumor progression and metastasis.
  • CXCR4 is a validated molecular target for cancer diagnostics and therapeutics.

Purpose of the Study:

  • To evaluate the CXCR4-targeting capability of 99mTc-labeled AMD3465, a small molecule CXCR4 antagonist.
  • To assess the potential of 99mTc-AMD3465 as a single photon emission computed tomography (SPECT) radiotracer for CXCR4-positive tumors.

Main Methods:

  • High-yield preparation and in vitro stability assessment of 99mTc-AMD3465.
  • In vitro cell binding assays using Chinese hamster ovary (CHO), MCF-7, and CHO-CXCR4 cell lines.
  • In vivo SPECT/CT imaging studies in nude mice bearing MCF-7 and CHO xenografts.

Main Results:

  • 99mTc-AMD3465 was synthesized with high radiochemical yield (>95%) and demonstrated stability in mouse serum for at least 4 hours.
  • Significant uptake of 99mTc-AMD3465 was observed in MCF-7 tumors compared to CXCR4-negative CHO tumors (P < 0.05).
  • Tumor uptake was specifically blocked by excess unlabeled AMD3465, confirming CXCR4-mediated targeting (P < 0.05).

Conclusions:

  • 99mTc-AMD3465 exhibits excellent in vitro and in vivo characteristics for targeting CXCR4.
  • This radiotracer demonstrates specific tumor uptake and retention in preclinical models.
  • 99mTc-AMD3465 holds potential as a SPECT imaging agent for evaluating CXCR4 expression in tumors.
Keywords:
AMD3465CXCR4SPECTTechnetium-99mtumor imaging

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