McMMAF (Maleimidocaproyl monomethylauristatin F) (Synonyms: Maleimidocaproyl monomethylauristatin F)

Mc-MMAF is a protective group-conjugated MMAF. MMAF is a more potent drug than Monomethyl auristatin E (MMAE), but is charged and relatively membrane-impermeable, is a potent tubulin inhibitor, is a toxin payload in antibody drug conjugate.Target:MMAF is a new auristatin derivative with a charged C-terminal phenylalanine that attenuates its cytotoxic activity compared to its uncharged counterpart, Monomethyl auristatin E (MMAE). Because of MMAF is highly toxic, it cannot be used as a drug itself. MMAF induces potent antitumor effects when conjugated via protease cleavable linkers to a monoclonal antibody targeting internalizing, tumor-specific cell surface antigens. The linker to the monoclonal antibody is stable in extracellular fluid, but is cleaved by cathepsin once the conjugate has entered a tumor cell, thus activating the anti-mitotic mechanism.

[1]. Polson AG, et al. Antibody-drug conjugates for the treatment of non-Hodgkin's lymphoma: target and linker-drug selection. Cancer Res. 2009 Mar 15;69(6):2358-2364. [2]. Jianmin Fang, et al. Anti-her2 antibody and conjugate thereof. US 20160304621 A1.