MMAF (Tubulin抑制剂)

化学名

(2S)-2-[[(2R,3R)-3-methoxy-3-[(2S)-1-[(3R,4S,5S)-3-methoxy-5-methyl-4-[methyl-[(2S)-3-methyl-2-[[(2S)-3-methyl-2-(methylamino)butanoyl]amino]butanoyl]amino]heptanoyl]pyrrolidin-2-yl]-2-methylpropanoyl]amino]-3-phenylpropanoic acid

简称

MMAF

别名

Monomethylauristatin F

中文名

一甲基澳瑞他汀

化学式

C₃₉H₆₅N₅O₈

分子量

731.96

CAS号

745017-94-1

纯度

98%

溶剂/溶解度

Water<1mg/ml; DMSO10mg/ml; Ethanol<1mg/ml

溶液配制

5mg加入0.68ml DMSO，或者每7.32mg加入1ml DMSO，配制成10mM溶液。SC2243-10mM用DMSO配制。

产品描述

Monomethylauristatin F(MMAF) is an antitubulin agent that inhibit cell division by blocking the polymerization of tubulin; lower cytotoxic activity than MMAE; antibody drug cytotoxin.

信号通路

Antibody-drug conjugates; Cell Cycle; DNA Damage

靶点

Tubulin

ADCs cytotoxin

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－

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IC50

－

－

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－

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体外研究

MMAF is a new auristatin derivative with a charged C-terminal phenylalanine that attenuates its cytotoxic activity compared to its uncharged counterpart, Monomethyl auristatin E (MMAE). Because ofmMAF is highly toxic, it cannot be used as a drug itself. mMAF induces potent antitumor effects when conjugated via protease cleavable linkers to a monoclonal antibody targeting internalizing, tumor-specific cell surface antigens. The linker to the monoclonal antibody is stable in extracellular fluid, but is cleaved by cathepsin once the conjugate has entered a tumor cell, thus activating the anti-mitotic mechanism.

体内研究

N/A

临床实验

N/A

特征

N/A

酶活性检测实验

方法

N/A

细胞实验

细胞系

N/A

浓度

N/A

处理时间

N/A

方法

N/A

动物实验

动物模型

N/A

配制

N/A

剂量

N/A

给药方式

N/A

产品编号

产品名称

包装

KL2243-10mM

MMAF (Tubulin抑制剂)

10mM×0.2ml

KL2243-5mg

MMAF (Tubulin抑制剂)

5mg

KL243-25mg

MMAF (Tubulin抑制剂)

25mg

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说明书

1份