Radioactive iodine marked protein binding ligand and application thereof
A technology of radioactive iodine and protein, which is applied in the direction of radioactive carriers, in vivo radioactive preparations, preparations for in vivo experiments, etc., can solve the problems of easy pollution of protein, easy to be affected by other factors, complicated preparation methods, etc., and improve pharmacokinetics The effects of biological properties, prolonged blood half-life, and simple labeling method
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Embodiment 1
[0043] 1.4-[ 131 I] Synthesis of IBA-NHS
[0044] Dissolve 1 g of 4-[(4-boronic acid phenyl) butyric acid (4-BBA) in 15 mL of DMF, add 981 mg of dicyclohexylcarbodiimide and 548 mg of N-hydroxysuccinimide, and stir at room temperature overnight . By-products were removed by filtration, and the filtrate was concentrated to obtain a white solid powder, the activated ester of 4-[(4-boronic acid phenyl)butanoic acid;
[0045] Take 1 mg of the activated ester (4-BBA-NHS) of 4-[(4-boronic acid phenyl) butyric acid, and add 50 μL of the catalyst of cuprous oxide and 1,10-phenanthroline mixed uniformly; add the above solution Into the air-dried radioactive iodine, shaking and reacting at room temperature for 30min, the labeled product 4-[ 131 I] IBA-NHS; add appropriate amount of Na 2 CO 3 It is hydrolyzed to obtain the target product 4-[ 131 I] IBA. The labeled final product was identified by HPLC, and its radioactive peak time could be compared with that of the stable albumin...
Embodiment 2
[0052] The following is the marker 4-[ 131 I] IBA, 4-[ 131 I]IBA-PEG or 4-[ 131 I] The performance measurement description of IBA-FA:
[0053] 1. Analysis and identification by TLC and HPLC
[0054] 4-[ 131 I] the TLC analysis system of IBA is as follows: sherwood oil: the system of ethyl acetate=1: 1 measures TLC to analyze with silica gel aluminum plate respectively at different time points; The system of physiological saline measures with polyamide film respectively at different time points TLC for analysis. 4-[ 131 I] the labeling rate of IBA is faster, has exceeded 99% in 10min; The radiochemical purity is high, greater than 95%; Stable in nature and difficult to decompose, until 24h it still exists stably in normal saline and acetonitrile solvent, TLC shows only A single peak appears, resulting in figure 1 shown.
[0055] 4-[ 131 I] The HPLC analysis system of IBA is as follows: Perkin-Elmer Series 200LC is equipped with Waters 2784 double absorption wavelength ...
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