Agents for cleaving labels from biomolecules in vivo
A labeling and pharmaceutical technology, applied in the direction of in vivo radioactive preparations, preparations for in vivo experiments, sugar derivatives, etc., can solve the problems of inconvenient methods, low efficiency, slow enzymatic cleavage methods, etc.
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[0921] General method:
[0922] All reagents, chemicals, materials and solvents were obtained from commercial sources and used as received, including undescribed nitrile starting compounds. All solvents are AR quality. [ 125 I] iodine, [ 111 In] indium and [ 177 Lu]lutetium chloride, and [ 89 Zr] zirconium oxalate solutions were purchased from PerkinElmer, Curium and IDB. Zeba desalting spin columns (7 and 40 kDa MW cut off, 0.5 mL) and Slide-A-Lyzer dialysis cassettes (20 kDa MW cut off) were purchased from Pierce Protein Research (Thermo Fisher Scientific). Mouse plasma was purchased from Innovative Research. 29-amino-3,6,9,12,15,18,21,24,27-nonanedioxan-1-ol (29-amino-3,6,9,12,15,18,21,24 , 27-nonaoxanonacosan-1-ol) was purchased from PurePEG. According to literature procedures [Westgen et al., Angew. Chem. Int. Ed. 2013, 52, 14112-14116]. Analytical thin layer chromatography was performed on Kieselgel F-254 precoated silica gel plates. Column chromatography was p...
example 1
[0924] Example 1: Synthesis of Conjugateable TCO-DOTA Constructs
[0925] Compound 1.1 (axial isomer) was prepared according to published methods [Rosin et al., Bioconjugate Chem. 2016, 27, 1697-1706].
[0926]
[0927] NHS-TCO-PEG4-DOTAGA (1.2):
[0928]
[0929] 4-[(14-Amino-3,6,9,12-tetraoxatetradec-1-yl)carbamoyl]-2-[4,7,10-tris(carboxymethyl)-1 ,4,7,10-Tetraazacyclododecan-1-yl]butyric acid hydrochloride (4-[(14-amino-3,6,9,12-tetraoxatetradecan-1-yl)carbamoyl]- 2-[4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododecan-1-yl]butanoic acid HCl salt) (18.0 mg, 25.9 μmol) and DiPEA (50.2 μL, 288 μmol) in H 2 The O solution was added to a solution of 1.1 (12.2 mg, 28.8 μmol) in acetonitrile, and the solution was stirred for 5 minutes. The reaction mixture was acidified before using 5% to 90% MeCN / H 2 Preparative RP-HPLC purification with an elution gradient of O (both containing 0.1% TFA) yielded compound 1.2 (10.0 mg, 9.98 μg, 39%) as a fluffy white powder after l...
example 2
[1019] Example 2: Synthesis of tetrazine cleaving agent
[1020] Tetrazine 2.15 and 2.16 were purchased from commercial sources. Tetrazines 2.13, 2.14, 2.17, 2.18 (10 kDa dextran) and 2.19 were prepared according to literature procedures [Westgen et al., Angew Chem Int Ed 2013, 53, 14112; Rosin et al., Bioconjug Chem 2016, 27, 1697; Fang et al., Angew Chem Int Ed 2016, 55, 14046], and tetrazine 2.20, 2.21 and 2.22 were prepared as described in WO2019212356 (wherein: compounds 2.12, 4.12, 4.28).
[1021]
[1022] 2,2'-(1,2,4,5-tetrazine-3,6-dimethyl)bis(pyridin-3-ol)(2,2'-(1,2,4,5-tetrazine- 3,6-diyl)bis(pyridin-3-ol))(2.1):
[1023]
[1024] 3-Hydroxypicolinonitrile (100 mg, 0.82 mmol) and hydrazine hydrate (280 μL, 4.9 mmol, 6 equiv) were stirred at 90° C. for 2 hours. Ethanol (4 mL) was added and the suspension was stirred at room temperature for 5 minutes. The suspension was filtered and the solids were washed with ethanol (5 x 2 mL). The solid was dried in vacuo...
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