产品描述

Monomethyl auristatin F, an antimitotic agent, inhibits cell division by blocking the polymerization of tubulin. 

靶点活性

Cytotoxicity( Karpas 299 cell) 

体外活性

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]. 

体内活性

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].

细胞实验

Cells are treated with serial dilutions of test molecules and incubated 4-6 days depending on cell line. Assessment of cellular growth and data reduction to generate IC50 values is done using Alamar Blue dye reduction assay[2]. 

别名

一甲基澳瑞他汀 F , MonoMethyl auristatin F , 

纯度

98%

分子量

731.98

分子式

C39H65N5O8

CAS No.

745017-94-1 

存储

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

溶解度

DMSO: Soluble

( < 1 mg/ml refers to the product slightly soluble or insoluble )

参考文献

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.

2. Lee JJ, et al. Enzymatic prenylation and oxime ligation for the synthesis of stable and homogeneous protein-drug conjugates for targeted therapy. Angew Chem Int Ed Engl. 2015 Oct 5;54(41):12020-4.

Note

For research use only .