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<p>Copper-64 (<sup>64</sup>Cu) and Copper-67 (<sup>67</sup>Cu) are promising theranostic isotopes for PET imaging and targeted radiotherapy. In this study, 2,2’-(1,2,4-Oxadiazole-3,5-diyl)di aniline (ODDA) was successfully radiolabeled with <sup>64+67</sup>Cu, achieving high radiolabeling yield (97.0 ± 0.8%) and excellent stability in serum over five days. The optimized radiolabeling conditions included a ligand concentration of 30&#xa0;µg, pH 4, a reaction time of 15&#xa0;min, and a temperature of 60&#xa0;°C. The biodistribution study in Ehrlich ascites carcinoma-bearing mice showed an initial tumor uptake of 7.8 ± 0.4%ID/g at 0.5&#xa0;h, peaking at 18.0 ± 0.3ID/g at 2&#xa0;h, confirming selective tumor accumulation. The log P value of -0.8 indicated a hydrophilic nature, leading to predominant renal clearance. Molecular docking studies showed strong binding to EGFR (-9.1&#xa0;kcal/mol) and VEGFR2 (-8.6&#xa0;kcal/mol), suggesting potential anticancer activity.</p>

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Radiolabeling and evaluation of 64+67Cu-2,2’-(1,2,4-Oxadiazole-3,5-diyl)di aniline as a theranostic agent for solid tumors

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2025年10月27日

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  • Mohamed A. Gizawy,
  • Mohammed Salah Ayoup,
  • Ahmad S. Kodous,
  • Mohamed Taha Abdelrahman,
  • M. A. Motaleb

摘要

Copper-64 (64Cu) and Copper-67 (67Cu) are promising theranostic isotopes for PET imaging and targeted radiotherapy. In this study, 2,2’-(1,2,4-Oxadiazole-3,5-diyl)di aniline (ODDA) was successfully radiolabeled with 64+67Cu, achieving high radiolabeling yield (97.0 ± 0.8%) and excellent stability in serum over five days. The optimized radiolabeling conditions included a ligand concentration of 30 µg, pH 4, a reaction time of 15 min, and a temperature of 60 °C. The biodistribution study in Ehrlich ascites carcinoma-bearing mice showed an initial tumor uptake of 7.8 ± 0.4%ID/g at 0.5 h, peaking at 18.0 ± 0.3ID/g at 2 h, confirming selective tumor accumulation. The log P value of -0.8 indicated a hydrophilic nature, leading to predominant renal clearance. Molecular docking studies showed strong binding to EGFR (-9.1 kcal/mol) and VEGFR2 (-8.6 kcal/mol), suggesting potential anticancer activity.