1369488-99-2Relevant articles and documents
A small bifunctional chelator that modulates Aβ42 aggregation
Zhang, Chaofeng,Gomes, Luiza M.F.,Zhang, Tonglu,Storr, Tim
, p. 78 - 82 (2018)
Multifunctional compounds that can modulate amyloid-β (Aβ) aggregation and interact with metal ions hold considerable promise as therapeutic agents for Alzheimer's disease (AD). Using the copper-catalyzed azide-alkyne cycloaddition reaction, a novel bifun
N-Succinimidyl 3-((4-(4-[18F]fluorobutyl)-1H-1,2,3-triazol-1-yl)methyl)-5-(guanidinomethyl)benzoate ([18F]SFBTMGMB): A residualizing label for 18F-labeling of internalizing biomolecules
Vaidyanathan, Ganesan,McDougald, Darryl,Choi, Jaeyeon,Pruszynski, Marek,Koumarianou, Eftychia,Zhou, Zhengyuan,Zalutsky, Michael R.
, p. 1261 - 1271 (2016/02/03)
Residualizing labeling methods for internalizing peptides and proteins are designed to trap the radionuclide inside the cell after intracellular degradation of the biomolecule. The goal of this work was to develop a residualizing label for the 18F-labeling of internalizing biomolecules based on a template used successfully for radioiodination. N-Succinimidyl 3-((4-(4-[18F]fluorobutyl)-1H-1,2,3-triazol-1-yl)methyl)-5-(bis-Boc-guanidinomethyl)benzoate ([18F]SFBTMGMB-Boc2) was synthesized by a click reaction of an azide precursor and [18F]fluorohexyne in 8.5 ± 2.8% average decay-corrected radiochemical yield (n = 15). An anti-HER2 nanobody 5F7 was labeled with 18F using [18F]SFBTMGMB ([18F]RL-I), obtained by the deprotection of [18F]SFBTMGMB-Boc2, in 31.2 ± 6.7% (n = 5) conjugation efficiency. The labeled nanobody had a radiochemical purity of >95%, bound to HER2-expressing BT474M1 breast cancer cells with an affinity of 4.7 ± 0.9 nM, and had an immunoreactive fraction of 62-80%. In summary, a novel residualizing prosthetic agent for labeling biomolecules with 18F has been developed. An anti-HER2 nanobody was labeled using this prosthetic group with retention of affinity and immunoreactivity to HER2.
Direct synthesis of organic azides from alcohols using 2-azido-1,3- dimethylimidazolinium hexafluorophosphate
Kitamura, Mitsuru,Koga, Tatsuya,Yano, Masakazu,Okauchi, Tatsuo
experimental part, p. 1335 - 1338 (2012/07/13)
Direct synthesis of organic azides from alcohols was developed. Azide transfer of 2-azido-1,3-dimethylimidazolinium hexafluorophosphate (ADMP) to alcohols proceeds to give the corresponding azides under mild reaction conditions, which were easily isolated because the byproducts are highly soluble in water. Georg Thieme Verlag Stuttgart · New York.
