Drug intelligence / Profile preview

MC-Val-Cit-PAB-MMAF

Development stage
Preclinical
Lead developer
Chongqing Sintaho Pharmaceutical
Modality
Classical Binding Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

MC-Val-Cit-PAB-MMAF is a linker-payload intermediate used in the construction of antibody-drug conjugates (ADCs). It consists of the cytotoxic agent monomethyl auristatin F (MMAF) conjugated to a maleimidocaproyl (MC) cap via a cathepsin B-cleavable valine-citrulline (Val-Cit) dipeptide and a self-immolative p-aminobenzyloxycarbonyl (PAB) spacer. MMAF is a potent tubulin inhibitor that disrupts microtubule polymerization, leading to cell cycle arrest and apoptosis. The Val-Cit-PAB linker system is designed to be stable in systemic circulation but rapidly cleaved by lysosomal proteases upon internalization into target cancer cells. Chongqing Sintaho provides this intermediate as part of its XDC toxin-linker platform for ADC development.

Other names
mc-vc-PAB-MMAFMaleimidocaproyl-valine-citrulline-p-aminobenzyloxycarbonyl-monomethyl auristatin F
02

Targets

TUBB (Tubulin (alpha and beta subunits))

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