782475-33-6

Upstream product

• 192650-25-2 6-(4-nitrophenyl)hexane-2,4-dione 
• 107-21-1 ethylene glycol 
• 123-54-6 acetylacetone 
• 100-11-8 1-bromomethyl-4-nitro-benzene 
• 7381-30-8 2,2,7,7-tetramethyl-3,6-dioxa-2,7-disilaoctane 
• 1363334-41-1 C₁₇H₂₁NO₆ 
• 16642-79-8 3-(4-nitrophenyl)propionic acid 
• 107324-93-6 3-(p-nitrophenyl)propanoyl chloride 

Downstream Products

• 1363334-43-3 C₂₆H₄₂N₃O₆⁽¹⁺⁾*Cl^(1-) 
• 1363334-40-0 C₂₂H₃₄N₃O₄⁽¹⁺⁾*Cl^(1-) 
• 1363334-42-2 C₂₁H₂₉NO₇ 
• 929088-03-9 3-[4-(2-{2-[2-(2-{2-[4-(3,5-dioxo-hexyl)-phenylcarbamoyl]-ethoxy}-ethoxy)-ethoxy]-ethoxy}-ethoxy)-phenyl]-N-[2'-(isoxazol-5-ylsulfamoyl)-4-oxazol-2-yl-biphenyl-2-ylmethyl]-N-methyl-propionamide 
• 929088-02-8 N-[4-(3,5-dioxo-hexyl)-phenyl]-3-{2-[2-(2-{2-[4-({[2'-(isoxazol-5-ylsulfamoyl)-4-oxazol-2-yl-biphenyl-2-ylmethyl]-methyl-carbamoyl}-methyl)-phenoxy]-ethoxy}-ethoxy)-ethoxy]-ethoxy}-propionamide 
• 929087-93-4 N-(2'-(isoxazol-5-ylsulfamoyl)-4-{2-[2-(2-{2-[2-(4-{2-[2-(2-methyl-[1,3]dioxolan-2-ylmethyl)-[1,3]dioxolan-2-yl]-ethyl}-phenylcarbamoyl)-ethoxy]-ethoxy}-ethoxy)-ethoxy]-ethoxy}-biphenyl-2-ylmethyl)-3,3,N-trimethyl-butyramide 
• 929087-89-8 3-(2-{2-[2-({[2'-(isoxazol-5-ylsulfamoyl)-4-oxazol-2-yl-biphenyl-2-ylmethyl]-methyl-carbamoyl}-methoxy)-ethoxy]-ethoxy}-ethoxy)-N-(4-{2-[2-(2-methyl-[1,3]dioxolan-2-ylmethyl)-[1,3]dioxolan-2-yl]-ethyl}-phenyl)-propionamide 
• 929087-81-0 N-[4-(2-{2-[2-(2-{2-[4-(3,5-dioxo-hexyl)-phenylcarbamoyl]-ethoxy}-ethoxy)-ethoxy]-ethoxy}-ethoxy)-2'-(isoxazol-5-ylsulfamoyl)-biphenyl-2-ylmethyl]-3,3,N-trimethyl-butyramide 
• 929087-92-3 3-{2-[2-(2-{2-[2-formyl-2'-(isoxazol-5-ylsulfamoyl)-biphenyl-4-yloxy]-ethoxy}-ethoxy)-ethoxy]-ethoxy}-N-(4-{2-[2-(2-methyl-[1,3]dioxolan-2-ylmethyl)-[1,3]dioxolan-2-yl]-ethyl}-phenyl)-propionamide 
• 929087-80-9 N-[4-(3,5-dioxo-hexyl)-phenyl]-3-(2-{2-[2-({[2'-(isoxazol-5-ylsulfamoyl)-4-oxazol-2-yl-biphenyl-2-ylmethyl]-methyl-carbamoyl}-methoxy)-ethoxy]-ethoxy}-ethoxy)-propionamide 
• 929087-94-5 3-[2-(2-{2-[2-(2-{2-[2-(4-{2-[2-(2-methyl-[1,3]dioxolan-2-ylmethyl)-[1,3]dioxolan-2-yl]-ethyl}-phenylcarbamoyl)-ethoxy]-ethoxy}-ethoxy)-ethoxy]-ethoxy}-ethoxy)-ethoxy]-propionic acid 
• 929088-01-7 3-(4-{2-[2-(2-{2-[2-(4-{2-[2-(2-methyl-[1,3]dioxolan-2-ylmethyl)-[1,3]dioxolan-2-yl]-ethyl}-phenylcarbamoyl)-ethoxy]-ethoxy}-ethoxy)-ethoxy]-ethoxy}-phenyl)-propionic acid 
• 929088-00-6 (4-{2-[2-(2-{2-[2-(4-{2-[2-(2-methyl-[1,3]dioxolan-2-ylmethyl)-[1,3]dioxolan-2-yl]-ethyl}-phenylcarbamoyl)-ethoxy]-ethoxy}-ethoxy)-ethoxy]-ethoxy}-phenyl)-acetic acid 

Relevant academic research and scientific papers

Synthesis of a novel analytical reagent for the determination of active sites for conjugation on a catalytic aldolase monoclonal antibody

An optimized and scalable synthesis of a novel analytical reagent for the determination of the number of active sites available for conjugation on a catalytic aldolase monoclonal antibody (mAb) is described. The original conditions suffered from lack of reproducibility, incomplete reactions, and required several chromatographies and lyophilizations that afforded material of low purity. A redesigned route and optimized protocols have been developed that eliminate the use of toxic and unsafe reagents such as HMPA and HATU. In addition, the number of chromatographies has been reduced to only one and time-consuming and energy-intensive lyophilizations are no longer required. The overall yield has been considerably improved from the original 4% to 20% after telescoping the last two steps of the synthesis and this new approach allowed for the preparation of material with higher chemical purity (≥99% vs the initial 90%) to meet specifications.

ANTI-ANGIOGENIC COMPOUNDS

The present invention provides AA targeting compounds which comprise AA targeting agent-linker conjugates which are linked to a combining site of an antibody. Various uses of the compounds are provided, including methods to treat disorders connected to abnormal angiogenesis.

Chemically programmed antibodies: Endothelin receptor targeting CovX-Bodies

Aryl sulfonamide-based endothelin antagonists were synthesized and covalently linked to the reactive lysine of the m38C2 antibody to create a series of CovX-Bodies. These chemically programmed antibodies behaved as potent endothelin receptor antagonists in vitro and had antitumor efficacy in a prostate cancer xenograft model which, on a molar basis, far exceeded the activity of the parent small molecule.

Anti-angiogenic compounds

The present invention provides AA targeting compounds which comprise AA targeting agent-linker conjugates which are linked to a combining site of an antibody. Various uses of the compounds are provided, including methods to treat disorders connected to abnormal angiogenesis.