Mal-N(Me)-C6-N(Me)-PNU-159682 is a drug-linker conjugate specifically designed for antibody-drug conjugates (ADCs). This compound utilizes the Mal-N(Me)-C6-N(Me) linker to selectively deliver the cytotoxic agent PNU-159682 to CD46-expressing cells. Upon entering these cells, the linker is cleaved by cathepsin B, resulting in the release of PNU-159682, which induces DNA damage and apoptosis. Notably, Mal-N(Me)-C6-N(Me)-PNU-159682 demonstrates significant tumor regression in patient-derived xenograft models of non-small cell lung cancer (NSCLC) and colorectal cancer (CRC).
Mal-N(Me)-C6-N(Me)-PNU-159682 is a drug-linker conjugate specifically designed for antibody-drug conjugates (ADCs). This compound utilizes the Mal-N(Me)-C6-N(Me) linker to selectively deliver the cytotoxic agent PNU-159682 to CD46-expressing cells. Upon entering these cells, the linker is cleaved by cathepsin B, resulting in the release of PNU-159682, which induces DNA damage and apoptosis. Notably, Mal-N(Me)-C6-N(Me)-PNU-159682 demonstrates significant tumor regression in patient-derived xenograft models of non-small cell lung cancer (NSCLC) and colorectal cancer (CRC).
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