Conjugation of doxorubicin to monoclonal anti-carcinoembryonic antigen antibody via novel thiol-directed cross-linking reagents

作者: Achilles Lau , Gervais Bérubé , Christopher H.J. Ford

DOI: 10.1016/0968-0896(95)00125-Z

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摘要: Abstract In order to improve the available methods produce an immunoconjugate use of longer heterobifunctional cross-linking reagents were investigated. Two new maleimidobenzoyl spacers have been synthesized in a one step process from 4-maleimidobenzoic acid. The fully characterized by their IR, 1H NMR, 13C NMR and mass spectra. These are selectively attached NH2-3′ daunosamine moiety doxorubicin. spacer-doxorubicin derivatives also spectrometry before coupling thiol groups thiolated anticarcinoembryonic antigen (CEA) monoclonal antibody (11-285-14). conjugates contain 1.51 – 3.44 molecules drug for each molecule (MAb).

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