782475-33-6Relevant articles and documents
Synthesis of a novel analytical reagent for the determination of active sites for conjugation on a catalytic aldolase monoclonal antibody
Magano, Javier,Farrand, Douglas,Haase, Jeffrey P.,Lovdahl, Michael,Maloney, Mark T.,Pozzo, Mark J.,Teixeira, John J.,Whritenour, David C.,Rizzo, John,Tumelty, David,Bhat, Abhijit,Bradshaw, Curt
scheme or table, p. 1385 - 1389 (2012/04/04)
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.
Chemically programmed antibodies: Endothelin receptor targeting CovX-Bodies
Doppalapudi, Venkata R.,Tryder, Nancy,Li, Lingna,Aja, Teresa,Griffith, David,Liao, Francesca-Fang,Roxas, Giovanni,Ramprasad, Mysore P.,Bradshaw, Curt,Barbas III, Carlos F.
, p. 501 - 506 (2007/10/03)
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.