PNU-159682 carboxylic acid

PNU-159682 Carboxylic Acid is a highly potent derivative of the anthracycline family and a notable ADC cytotoxin frequently used as an ADC payload in the development of antibody-drug conjugates. Its mechanism of action involves intercalation into DNA and inhibition of topoisomerase II, which induces double-strand DNA breaks and triggers rapid apoptosis in rapidly dividing tumor cells. The carboxylic acid modification enhances its conjugation compatibility with antibody linkers, providing improved stability and versatility in ADC design.

Within antibody-drug conjugates, PNU-159682 Carboxylic Acid is typically attached to monoclonal antibodies via cleavable or non-cleavable linker chemistries. This ensures that the payload remains inactive in systemic circulation and is selectively released inside tumor cells after internalization and enzymatic processing. The ADC-specific delivery mechanism allows potent cytotoxicity directly at the tumor site, minimizing off-target toxicity and enhancing the therapeutic index. Its extremely high potency makes it effective even at low drug-to-antibody ratios (DARs), which is critical for precision oncology applications.

Applications of PNU-159682 Carboxylic Acid include its use in preclinical and clinical ADC candidates targeting both hematologic malignancies and solid tumors, such as leukemia, lymphoma, breast cancer, and lung cancer. Its chemical structure supports conjugation with various linker technologies, optimizing stability, intracellular release, and overall ADC performance. Researchers leverage PNU-159682 Carboxylic Acid to develop next-generation ADCs with superior antitumor efficacy, tumor selectivity, and reduced systemic side effects.