货号：M3727

储存条件：粉末-20°C可保存3年；液体-80°C可保存12月。

产品描述

MMAF is a potent auristatin-derived antineoplastic agent, working by inhibition of tubulin polymerization. Different from its analogue MMAE, it has attenuated cytotoxicity due its charged C-terminal phenylalanine. MMAF exhibited cytotoxicity in Karpas 299, H3396, 786-O and Caki-1 cells with IC50 values of 119nM, 105nM, 257nM and 200nM after 96-hour treatment. For the high toxicity of MMAF, it is usually used as the payload of ADCs (antibody-drug conjugates), such as combination with antibody-drug conjugates such as vorsetuzumab mafodotin or SGN-CD19A. Through the link to specific antibody, the selectivity and potency of MMAF could be proved. For example, the ADC cAC10-L4-MMAF₄ (anti-CD30) showed cytotoxicity to Karpas 299 cells with IC50 value of 0.065 nM (compared with 119nM, MMAF alone). Intravenous injection with cAC10-L4-MMAF₄ at dose of 2mg/kg almost suppressed the median tumor growth in SCID mice xenograft Karpas 299 human ALCL tumors. And the survival was significantly prolonged when the mice were dosed of 8mg/kg cAC10-L4-MMAF₄.

作用机制

MMAF is an auristatin derivate which can inhibi tubulin polymerization and destabilize microtubule structure.

产品信息