Radiosynthesis and evaluation of a 68Ga-labeled brominated benzamide derivative for detection of melanoma in small animals
Radiosynthesis and evaluation of a 68Ga-labeled brominated benzamide derivative for detection of melanoma in small animals
홍다경(Gyeongsang National University); 이채원(Gyeongsang National University); 송보름(Gyeongsang National University); 김은수(Gyeongsang National University); 서예진(Gyeongsang National University); 김지유(CNCure Biotech); 정우경(CNCure Biotech); 권승영(Chonnam National University Medical School and Hwasun Hospital); 김동연(Gyeongsang National University); 표아영(Gyeongsang National University)
46권 5호, 540~546쪽
초록
Malignant melanoma has the highest mortality rate of any skin cancer due toits aggressive nature and high potential for metastasis, and early diagnosis iscritical for improving outcomes because of the limited treatment options availablefor patients. We synthesized a brominated benzamide derivative labeledwith 68Ga and evaluated its biological properties as an imaging agent fordetecting melanoma using positron emission tomography (PET). The eluted68Ga was dissolved in 1.0 M NaOAc buffer and labeled with the synthesizedprecursor. The radiochemical yield and radiochemical purity of the 68Ga chelationcomplex were confirmed by radio-thin layer chromatography. In vitrouptake was measured in the murine melanoma cell line (B16F10), and in vivostudies were performed with B16F10-bearing mice. The total radiochemicalyield was over 95% (n > 3), and the radiochemical purity was above 98%. The68Ga-labeled compound showed high uptake in B16F10 cells activated with Ltyrosine(2 mM) (6561.48 ± 1067.52 counts per minute [CPM] at 30 min,8987.03 ± 888.64 CPM at 60 min). The labeled compound allowed visualizationof B16F10 xenografts on microPET at 60 min after intravenous injection (tumoruptake: 1.20 ± 0.20% ID/g at 30 min, 0.91 ± 0.24% ID/g at 60 min). Theseresults suggest that 68Ga-labeled 2,20,200,2000-(2-(4-(3-(2-((2-(5-bromopicolinamido)ethyl)(methyl)amino)ethyl)thioureido)benzyl)-1,4,7,10-tetraazacyclododecane-1,4,7,10-tetrayl)tetraacetic acid (68Ga-MI-0202E1) has potential as a PETimaging probe for the detection of melanoma.
Abstract
Malignant melanoma has the highest mortality rate of any skin cancer due toits aggressive nature and high potential for metastasis, and early diagnosis iscritical for improving outcomes because of the limited treatment options availablefor patients. We synthesized a brominated benzamide derivative labeledwith 68Ga and evaluated its biological properties as an imaging agent fordetecting melanoma using positron emission tomography (PET). The eluted68Ga was dissolved in 1.0 M NaOAc buffer and labeled with the synthesizedprecursor. The radiochemical yield and radiochemical purity of the 68Ga chelationcomplex were confirmed by radio-thin layer chromatography. In vitrouptake was measured in the murine melanoma cell line (B16F10), and in vivostudies were performed with B16F10-bearing mice. The total radiochemicalyield was over 95% (n > 3), and the radiochemical purity was above 98%. The68Ga-labeled compound showed high uptake in B16F10 cells activated with Ltyrosine(2 mM) (6561.48 ± 1067.52 counts per minute [CPM] at 30 min,8987.03 ± 888.64 CPM at 60 min). The labeled compound allowed visualizationof B16F10 xenografts on microPET at 60 min after intravenous injection (tumoruptake: 1.20 ± 0.20% ID/g at 30 min, 0.91 ± 0.24% ID/g at 60 min). Theseresults suggest that 68Ga-labeled 2,20,200,2000-(2-(4-(3-(2-((2-(5-bromopicolinamido)ethyl)(methyl)amino)ethyl)thioureido)benzyl)-1,4,7,10-tetraazacyclododecane-1,4,7,10-tetrayl)tetraacetic acid (68Ga-MI-0202E1) has potential as a PETimaging probe for the detection of melanoma.
- 발행기관:
- 대한화학회
- 분류:
- 화학