CD25 targeting polypeptide, molecular probe and application
A technology targeting peptides and molecular probes, applied in peptides, peptide preparation methods, organic chemistry, etc., can solve problems such as slow removal speed, difficult imaging effect, patient pain, etc., achieve high affinity, and improve signal-to-noise ratio , the effect of high intake
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Embodiment 1
[0050] Preparation of DA-1 RFK(GGG-DOTA)FY[OBn];
[0051] .
[0052] (1) Resin swelling, put 2-CTC resin (50 mg, 0.015 mmol~0.15 mmol) into the reaction tube, add DCM (4 mL), and shake for 30 min. (2) Connect the first amino acid, filter out the solvent through sand core, add 2 times molar excess of Fmoc-L-Tyr(Bzl)-OH (148 mg, 0.30 mmol), add DMF to dissolve, and then add 10 times molar Excess DIEA (261 μL, 1.50 mmol) was shaken for 60 min. Block with methanol. (3) Deprotection, remove methanol, add 20% piperidine DMF solution (3 mL) for 5 min, remove and add 20% piperidine DMF solution (3 mL) for 15 min. (4) Detection, remove the piperidine solution, take more than ten resins, wash with ethanol three times, add detection reagent for detection, heat at 105℃-110℃ for 5min, and it turns dark blue as a positive reaction. (E) Wash, DMF (4 mL) twice, DCM (4 mL) twice, DMF (4 mL) twice. (VI) Condensation, adding the next Fmoc-protected amino acid Fmoc-L-Phe-OH (116 mg, 0.30 ...
Embodiment 2
[0054] Preparation of DA-3 DOTA-(PEG)2-RFKFYE.
[0055] .
[0056] (1) Resin swelling: Put 2-CTC resin (50 mg, 0.015 mmol~0.15 mmol) into the reaction tube, add dichloromethane (4 mL), and shake for 30 min. (2) Connection of the first amino acid: The solvent was filtered off through a sand core, and a 2-fold molar excess of N-fluorenemethoxycarbonyl-L-glutamic acid-γ-tert-butyl ester monohydrate (133 mg, 0.30 mmol) was added, Add DMF to dissolve, then add 10-fold molar excess DIEA (261 μL, 1.50 mmol), shake for 60 min, and block with methanol. (3) Deprotection: remove methanol, add 20% piperidine DMF solution (3 mL), stir for 5 min, remove the solvent, add 20% piperidine DMF solution (3 mL), and stir for 15 min. (4) Detection: remove the piperidine solution, take more than ten resins, wash with ethanol three times, add detection reagent for detection, heat at 105 ℃-110 ℃ for 5 min, and it turns dark blue as a positive reaction. (5) Washing: DMF (4 mL) twice, DCM (4 mL) tw...
Embodiment 3
[0058] Preparation of DA-6 DOTA-(PEG)2-RFrFY:
[0059] .
[0060](1) Resin swelling: Put 2-CTC resin (50 mg, 0.015 mmol~0.15 mmol) into the reaction tube, add dichloromethane (4 mL), and shake for 30 min. (2) First amino acid connection: filter out the solvent through sand core, add 2 times molar excess of Fmoc-O-tert-butyl-L-tyrosine (137.70 mg, 0.30 mmol), add DMF to dissolve, and then add 10 times more Molar excess of DIEA (261 μL, 1.50 mmol), shaken for 60 min, and blocked with methanol. (3) Deprotection: remove methanol, add 20% piperidine DMF solution (3 mL), stir for 5 min, remove the solvent, add 20% piperidine DMF solution (3 mL), and stir for 15 min. (4) Detection: Remove the piperidine solution, take more than ten resins, wash with ethanol three times, add detection reagents for detection, heat at 105℃-110℃ for 5 minutes, and turn dark blue as a positive reaction. (5) Washing: DMF (4 mL) twice, DCM (4 mL) twice, DMF (4 mL) twice. (VI) Condensation: Add 2 times...
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