Mal-PEG2-VCP-eribulin

Mal-PEG2-VCP-eribulin is a specialized payload-linker intermediate designed for the synthesis of antibody-drug conjugates (ADCs), developed by Chongqing Sintaho. It features eribulin, a synthetic macrocyclic ketone analogue of the marine natural product halichondrin B, as the cytotoxic payload. Eribulin exerts its therapeutic effect by inhibiting the growth phase of microtubules without affecting the shortening phase, leading to the sequestration of tubulin into non-productive aggregates and subsequent G2/M cell-cycle arrest. The linker system comprises a protease-cleavable Valine-Citrulline-PAB (VCP) moiety, which ensures stable circulation and selective release of the payload within the lysosomal compartment of target cells upon cleavage by enzymes such as cathepsin B. A short PEG2 (polyethylene glycol) spacer is incorporated to enhance the hydrophilicity and solubility of the conjugate, while a terminal maleimide (Mal) group allows for site-specific conjugation to cysteine residues on a targeting antibody or protein. This molecule serves as a modular building block for the construction of novel ADCs targeting various malignancies.

Other names

Mal-PEG2-Val-Cit-PAB-eribulinMal-PEG-2-Val-Cit-PAB-eribulinMal-PEG 2-Val-Cit-PAB-eribulinMaleimide-PEG2-Val-Cit-PAB-eribulinMaleimide-PEG-2-Val-Cit-PAB-eribulinMaleimide-PEG 2-Val-Cit-PAB-eribulin