val-cit-pab-exatecan

val-cit-pab-exatecan is a linker-payload intermediate designed for the construction of antibody-drug conjugates (ADCs). It consists of the potent topoisomerase I inhibitor exatecan conjugated to a cathepsin B-cleavable valine-citrulline (Val-Cit) dipeptide linker with a para-aminobenzyloxycarbonyl (PAB) self-immolative spacer. Upon internalization of the ADC into target cancer cells, the Val-Cit linker is enzymatically cleaved by lysosomal proteases, triggering the release of the exatecan payload. Exatecan then inhibits DNA topoisomerase I, leading to DNA strand breaks and apoptosis. This specific construct is part of Chongqing Sintaho's portfolio of XDC (any-drug conjugate) components.

Other names

valine-citrulline-p-aminobenzyloxycarbonyl-exatecan