Prostate cancer PET diagnostic reagent 68Ga-DOTA-ANCP-PSMA and preparation method and application thereof
A technology of DOTA-ANCP-PSMA and 68ga-dota-ancp-psma, which is applied in the field of medicine, can solve the problems of not being protected by patents and not applicable to targeted therapy, and achieves fast labeling speed, high labeling rate and good stability Effect
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Embodiment 1
[0041] This embodiment provides a prostate cancer PET diagnostic reagent 68 The preparation method of Ga-DOTA-ANCP-PSMA, described method comprises the steps:
[0042] (S1) Synthesizing the precursor compound DOTA-ANCP-PSMA by solid phase synthesis;
[0043] Preparation of compound 3
[0044] The synthetic route is shown below. Using Fmoc-Lys(Dde)-Wang Resin (compound 1) as the starting material, weigh 3g of the raw material with a substitution degree of 0.3mmol / g, add it to the reactor, add DMF, and soak for 30min. Then drain the DMF, add 3 times the volume of 20% Pip / DMF, and fill with nitrogen gas to remove Fmoc, react for 30 minutes, drain the 20% Pip / DMF, wash with DMF 5 times, and the ninhydrin detection shows dark blue. Add N,N'-succinimidyl carbonate (DSC), N,N-diisopropylethylamine (DIPEA) and 4-dimethylaminopyridine (DMAP) in proportion, and the input ratio is resin:DSC: DIPEA:DMAP=1:6:12:1, add an appropriate amount of DMF, and react for 1 h under nitrogen protec...
Embodiment 2
[0058] In vitro stability assay:
[0059] 68 The radiochemical stability of Ga-DOTA-ANCP-PSMA was carried out in two systems of calf serum and phosphate buffer. PBS method: place in 0.5mL phosphate buffer (PBS, pH=7.4), place at 37°C, incubate for 30, 60, 90, 120, 150min, then use HPLC to measure its radiochemical purity to determine its in vitro stability. Serum method: place in 0.5mL calf serum solution, incubate at pH=7, 37°C. When incubated for 30, 60, 90, 120, and 150 min, the radiochemical purity was determined by HPLC to determine its in vitro stability.
[0060] according to Figure 4 The results showed that from 30 minutes to 150 minutes, the radiochemical purity decreased slightly, but the stability remained above 95%. 68 Ga-DOTA-ANCP-PSMA has good stability in PBS system. In the serum system, from 30 minutes onwards, the radiochemical purity decreased to a certain extent, and the radiochemical purity was lower than 95% in 1.5 hours. 68 The stability of Ga-DOT...
Embodiment 3
[0062] Measurement of lipid-water partition coefficient:
[0063] Mark 68Ga-DOTA-ANCP-PSMA was separated and purified by Sep-Pak C18 Cartridge, and eluted with 95% ethanol. The obtained marker was blown dry by dry nitrogen, and the obtained marker was dissolved in a 1.5mL EP tube (about 3.7MBq) using the same volume (0.5mL: 0.5mL) of n-octanol and phosphate buffer solution (pH=7.4) middle. Fully shake for 5 minutes, and centrifuge the layers in a centrifuge for 5 minutes at a speed of 2000 rpm. Take 100uL each of the organic phase and the aqueous phase in 1mL EP tubes, measure their radioactive counts in the well-type γ detector, and calculate the lipid-water partition coefficient P from the ratio of the radioactive counts of the organic phase and the aqueous phase. P=log(N O / N W )(N O and N W are the counts of the organic and aqueous phase samples, respectively). The operation was repeated 3 times, and the average value was taken as the lipid-water partition coeffici...
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