2022年7月1日 · Fully automated synthesis of the theranostic pair [90 Y]Y/ [68 Ga]Ga-FAPI-46 was achieved on the Trasis EasyOne synthesizer with a radiochemical yield of 88 ± 7% and 56 ± 5% with a radiochemical purity of >99%. Stability experiments showed a durability for [68 Ga]Ga-FAPI-46 within 4 h and for [90 Y]Y-FAPI-46 within 24 h.

2021年4月16日 · A fully automated synthesis of [177Lu]Lu-FAPI derivatives was achieved on the Modular Lab Eazy (ML Eazy) with high radiochemical yield ([177Lu]Lu-FAPI-04; 88% ± 3, [177Lu]Lu-FAPI-46; 86% ± 3). Chromatographic analysis indicated the formation of radiosynthesis with an absolute radiochemical purity (99%).

2024年4月1日 · Radio-thin layer chromatography (TLC) analyses were performed using 2 iTLC-SG strips (2 cm × 10 cm). A small drop of [68 Ga]Ga-FAPI-46 was placed on each strip 2 cm above the base line. The first strip was placed in a development chamber containing aqueous 1 M ammonium acetate in methanol (1:1) as mobile phase (conditions A); the second strip ...

2022年7月29日 · The recent development of quinoline-based radiotracers, which act as fibroblast activation protein inhibitors (FAPIs), has shown promising preclinical and clinical advantages. [68 Ga]Ga-FAPI-46 is a new radiotracer for in vivo detection of the fibroblast activation protein by positron emission tomography (PET).

2022年7月29日 · The synthesis of [68 Ga]Ga-FAPI-46 was performed by mixing 50 µg of the FAPI-46 precursor with the [68 Ga]GaCl 3 solution directly eluted from the generator at 90 °C and continued heating for 4 min.

2023年8月11日 · [68Ga]Ga-FAPI-46 is a radiolabelled fibroblast activation protein inhibitor that selectively binds to fibroblast activation protein (FAP), which is overexpressed by cancer-associated fibroblasts (CAFs) in the tumour microenvironment.

2022年7月29日 · Background The recent development of quinoline-based radiotracers, which act as fibroblast activation protein inhibitors (FAPIs), has shown promising preclinical and clinical advantages....

2024年4月1日 · Radiochemical purity (RCP) of [68Ga]Ga-FAPI-46 was analyzed by ascending chromatography using either ITLC-SG strip and 0.1 M ammonium acetate and methanol (1:1) solution or TLC and 1 M sodium citrate (pH = 5.5), and Sep-Pak C18 cartridge. Radiochemical stability was assessed through UHPLC analysis.

2021年3月3日 · In this work, a fully-automated [¹⁷⁷Lu]Lu-FAPI synthesis has been well designed for the first time using commercially available synthesis module. In addition to the development of an automated...

近年来，基于喹啉设计的小分子fap抑制剂(fapinhibitor，fapi)显示出优秀的fap亲和力，多种68ga-fapi也在动物实验中显示了高度的肿瘤摄取和快速的体内清除，非常适用于体内成像，目前国内临床各家医院采用的是金属核素68ga标记fapi的化合物，由于68ga由发生器产生 ...