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CC-1065 is a potent antitumor antibiotic and DNA-alkylating agent originally isolated from the bacterium *Streptomyces zelensis*. It belongs to the duocarmycin class of compounds and is characterized by its ability to bind covalently to the N3 position of adenine within the minor groove of DNA, thereby disrupting DNA synthesis. While it exhibits extreme cytotoxicity—approximately 400 times more potent than doxorubicin—its clinical development as a monotherapy was halted due to severe systemic toxicity, specifically a 'delayed lethality' syndrome observed in preclinical models. Currently, CC-1065 and its derivatives are primarily utilized as cytotoxic payloads in the development of antibody-drug conjugates (ADCs) and in antibody-directed enzyme prodrug therapy (ADEPT) to leverage their potency while minimizing off-target effects.
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