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Monomethyl auristatin E
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。
Monomethyl auristatin E图片
CAS NO:474645-27-7
包装与价格:
包装价格(元)
10 mg电议
25 mg电议
50 mg电议
100 mg电议

产品名称
一甲基澳瑞他汀E
Vedotin
MMAE
产品介绍
Monomethyl auriSTATin E 是海兔毒素 10 的合成衍生物,是一种抗有丝分裂剂,通过阻断微管蛋白的聚合来抑制细胞分裂,并且还具有抑制抗体-药物偶联物的活性。

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.

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)

Cas No.

474645-27-7

分子式

C39H67N5O7

分子量

717.993

别名

一甲基澳瑞他汀E;Vedotin;MMAE

储存和溶解度

DMSO:71.8 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years