瀏覽量: 148
- 產(chǎn)品名稱: MMAF
- 產(chǎn)品貨號(hào): CS00039
- 貨期: 現(xiàn)貨
- 價(jià)格與訂購: 450
- 數(shù)量:
- 規(guī)格: 10mg
- 產(chǎn)品信息
- 如何訂購
產(chǎn)品描述
Monomethyl auristatin F, an antimitotic agent, inhibits cell division by blocking the polymerization of tubulin.
靶點(diǎn)活性
Cytotoxicity( Karpas 299 cell)
體外活性
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].
體內(nèi)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].
細(xì)胞實(shí)驗(yàn)
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].
別名
一甲基澳瑞他汀 F , MonoMethyl auristatin F ,
純度
98%
分子量
731.98
分子式
C39H65N5O8
CAS No.
745017-94-1
存儲(chǔ)
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 )
參考文獻(xiàn)
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 .
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