Monomethyl auristatin E

Monomethyl auristatin E (MMAE; SGD-1010) is a synthetic derivative of dolastatin 10 and functions as a potent mitotic inhibitor by inhibiting tubulin polymerization. MMAE is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) to treat several different cancer types. IC50 & Target:Microtubule^[1] In Vitro: Monomethyl auristatin E (MMAE) is efficiently released from SGN-35 within CD30⁺ cancer cells and, due to its membrane permeability, is able to exert cytotoxic activity on bystander cells^[1].
MMAE sensitizes colorectal and pancreatic cancer cells to IR in a schedule and dose dependent manner correlating with mitotic arrest. Radiosensitization is evidenced by decreased clonogenic survival and increased DNA double strand breaks in irradiated cells^[2]. In Vivo: Monomethyl auristatin E (MMAE) in combination with IR results in tumor growth delay, tumor-targeted ACPP-cRGD-MMAE with IR produces a more robust and significantly prolongs tumor regression in xenograft models^[2].