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D8-MMAF
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
D8-MMAF图片
规格:98%
分子量:740.01
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
D8-MMAF是MMAF的氘代形式。
货号:ajcx13838
CAS:N/A
分子式:C39H57D8N5O8
分子量:740.01
溶解度:Soluble in DMSO
纯度:98%
存储:Store at -20°C
库存:现货

Background:

D8-MMAF is a deuterated form of MMAF, which is a microtubule disrupting agent. IC50: 119 nM (Cytotoxicity, Karpas 299 cell), 105 nM (Cytotoxicity, H3396 cell), 257 nM (Cytotoxicity, 786-O cell), 200 nM (Cytotoxicity, Caki-1, cell)[1]

MMAF shows in vitro cytotoxicity against a panel of cell lines. The IC50 values for Karpas 299, H3396, 786-O and Caki-1 are 119, 105, 257, and 200 nM, respectively. Targeted MMAF is much more potent than the free drug, and that cAC10 conjugates of MMAF display pronounced activities. On a molar basis, the cAC10-L1-MMAF4 is an average of over 2200-fold more potent than free MMAF and is active on all the CD30-positive cell lines tested[1].

The maximum tolerated dose in mice of MMAF (>16 mg/kg) is much higher than MMAE (1 mg/kg). cAC10-L1-MMAF4 has an MTD of 50 mg/kg in mice and 15 mg/kg in rats. The corresponding cAC10-L4-MMAF4 ADC was much less toxic, having MTDs in mice and rats of >150 mg/ kg and 90 mg/kg in rats, respectively[1].

[1]. Doronina SO, et al. Enhanced activity of monomethylauristatin F through monoclonal antibody delivery: effects of linker technology on efficacy and toxicity. Bioconjug Chem. 2006 Jan-Feb;17(1):114-24.