1027359-36-9

Upstream product

• 72080-83-2 2-benzyloxycarbonylaminoethylamine 
• 598-21-0 2-Bromoacetyl bromide 
• 22118-09-8 2-bromoacetyl chloride 

Downstream Products

• 1037795-38-2 C₃₄H₄₉N₇O₈ 
• 1027359-40-5 tri-tert-butyl 2,2',2''-(10-(2-((2-(((benzyloxy)carbonyl)amino)ethyl)amino)-2-oxoethyl)-1,4,7,10-tetraazacyclododecane-1,4,7-triyl)triacetate 
• 1037795-42-8 C₃₀H₄₁N₇O₈ 
• 1277166-08-1 {4,10-bis-[(2-benzyloxycarbonylamino-ethylcarbamoyl)methyl]-7-tert-butoxycarbonylmethyl-1,4,7,10-tetraaza-cyclododec-1-yl}-acetic acid tert-butyl ester 

Relevant academic research and scientific papers

Optimization of Artificial Siderophores as 68Ga-Complexed PET Tracers for in Vivo Imaging of Bacterial Infections

The diagnosis of bacterial infections at deep body sites benefits from noninvasive imaging of molecular probes that can be traced by positron emission tomography (PET). We specifically labeled bacteria by targeting their iron transport system with artificial siderophores. The cyclen-based probes contain different binding sites for iron and the PET nuclide gallium-68. A panel of 11 siderophores with different iron coordination numbers and geometries was synthesized in up to 8 steps, and candidates with the best siderophore potential were selected by a growth recovery assay. The probes [68Ga]7 and [68Ga]15 were found to be suitable for PET imaging based on their radiochemical yield, radiochemical purity, and complex stability in vitro and in vivo. Both showed significant uptake in mice infected with Escherichia coli and were able to discern infection from lipopolysaccharide-triggered, sterile inflammation. The study qualifies cyclen-based artificial siderophores as readily accessible scaffolds for the in vivo imaging of bacteria.

CHEMICAL LINKERS AND CLEAVABLE SUBSTRATES AND CONJUGATES THEREOF

The present disclosure provides drug-ligand conjugates and drug-cleavable substrate conjugates that are potent cytotoxins. The disclosure is also directed to compositions containing the drug-ligand conjugates, and to methods of treatment using them.

Bifunctional ligands based on the DOTA-monoamide cage

Efficient routes to DOTA-monoamide ligands bearing amino, hydroxyl, aldehyde and maleimido groups are described. These functional groups, which can be spaced at will from the coordination cage, will readily react with suitable groups of targeting moieties

CHEMICAL LINKERS WITH SINGLE AMINO ACIDS AND CONJUGATES THEREOF

The present disclosure provides drug-ligand conjugates that are potent cytotoxins and include a linker between the drug and ligand where the linker has a single amino acid. The disclosure is also directed to compositions containing the drug-ligand conjugates, and to methods of treatment using them.