Results in Chemistry (May 2025)
The 68Ga-labeled chlorinated benzamide derivative: A novel PET imaging probe for detection of melanoma
Abstract
The benzamide structure is known for its ability to target melanin, a specific biomarker of melanoma. Therefore, we developed a new chlorinated benzamide structure for the detection of melanoma on positron emission tomography (PET). The derived benzamide structure was combined with a specific amine structure and labeled with the radioactive isotope 68Ga by incorporating the chelator p-SCN-Bn-DOTA (2-(4-isothiocyanatobenzyl)-1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid) for PET imaging. In vitro uptake was measured in the B16F10 mouse melanoma cell line, and in vivo studies were performed with B16F10-bearing mice. The radiochemical yield of chlorinated benzamide derivative was over 95 % (n > 3) at 90 °C for 10 min at pH 5.5, and the radiochemical purity exceeded 98 %. Cell uptake of labeled compound was significantly higher in melanin-expressing cells than in non-melanin-expressing cells. Furthermore, this compound successfully imaged B16F10 xenografts on microPET imaging. The chlorinated benzamide derivative successfully chelated 68Ga and specifically imaged melanoma and may therefore have potential as an imaging agent for malignant melanoma with melanin overexpression.
