Mc-MMAF是由高效微管抑制剂MonomethylauristatinF(MMAF)与保护基团maleimidocaproyl偶联而成。MMAF(一甲基澳瑞他汀F)为抗微管蛋白化合物，能通过阻断微管聚合抑制细胞分裂，较MMAE毒性低，可用于抗体偶联药物（ADC）。
CAS：863971-19-1
分子式：C49H76N6O11
分子量：925.16
纯度：98%
存储：Store at -20°C

Background:

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.