产品描述

Monomethyl auristatin E (MMAE), an antimitotic agent, inhibits cell division by blocking the polymerization of tubulin and also has inhibition of antibody-drug conjugates (ADCs) activity. 

靶点活性

microtubule

体外活性

When coupled to cAC10, MMAE shows selective cytotoxicity in CD30+ cells, and induces G2/M-phase growth arrest and cell death through the induction of apoptosis. [1] When coupled to anti-CD79b antibody, anti–CD79b-vcMMAE has very potent and broad activity across a large panel of NHL cell lines in vitro. [2] When coupled to anti-HER2 antibody, hertuzumab-vc-MMAE can also be effectively internalized and potently kill HER2 over-expressing tumor cells. [3] .

体内活性

In the Karpas 299 ALCL model, cAC10-vcMMAE (1 mg/kg, i.v.) induces complete, durable tumor regression, while free MMAE (0.36 mg/kg) doesn't produce detectable antitumor activity. [1] In mouse xenograft models of NHL, anti–CD79b-vcMMAE (7 mg/kg, p.o.) strikingly results in sustained complete tumor remission. [2] 

细胞实验

Cytotoxicity is measured using Alamar Blue dye reduction assay according to the manufacturer's directions. Briefly, a 40% solution (wt/vol) of Alamar Blue is freshly prepared in complete media just before cultures are added. Ninety-two hours after drug exposure, Alamar Blue solution is added to cells to constitute 10% culture volume. Cells are incubated for 4 hours, and dye reduction is measured on a Fusion HT fluorescent plate reader (Packard Instruments, Meriden, CT). (Only for Reference) Cell lines: CD30+ Karpas 299 cells .

别名

一甲基澳瑞他汀E , MMAE , Vedotin , 一甲基澳瑞他汀E , MMAE Vedotin 

纯度

98%

分子量

717.98 

分子式

C39H67N5O7

CAS No.

474645-27-7 

存储

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

溶解度

DMSO: 71.8 mg/mL (100 mM)

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

参考文献

1. Francisco JA, et al. Blood. 2003, 102(4), 1458-1465.

2. Dornan D, et al. Blood. 2009, 114(13), 2721-2729.

3. Yao X, et al. Breast Cancer Res Treat. 2015, 153(1), 123-133.

Note

For research use only .