McMMAF 是一种保护基团共轭的 MMAF。它是一种具有马来酰亚胺基己酰基接头(MC 接头)的 MMAF 衍生物, MMAF 是一种有效的微管蛋白聚合抑制剂。它可与抗体或其他蛋白质或生物聚合物结合。
产品描述
McMMAF is a protective group-conjugated MMAF. MMAF is a potent tubulin polymerization inhibitor.It is a MMAF derivative having a Maleimidocaproyl linker (MC linker), which is ready to conjugate to antibody or other proteins or biopolymers. Mafodotin is a useful agent for make antibody drug conjugate (ADC) for targeted drug delivery.
体外活性
MMAF induces potent antitumor effects when conjugated via protease cleavable linkers to a monoclonal antibody targeting internalizing, tumor-specific cell surface antigens. 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). It cannot be used as a drug itself because MMAF is highly toxic. 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.
Cas No.
863971-19-1
分子式
C49H76N6O11
分子量
925.16
别名
Maleimidocaproyl monomethylauristatin F
储存和溶解度
DMSO:100 mg/mL (108.09 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years