化學(xué)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

簡稱

MMAF

別名

Monomethylauristatin F

中文名

一甲基澳瑞他汀

化學(xué)式

C₃₉H₆₅N₅O₈

分子量

731.96

CAS號

745017-94-1

純度

98%

溶劑/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。

產(chǎn)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.

信號通路

Antibody-drug conjugates; Cell Cycle; DNA Damage

靶點(diǎn)

Tubulin

ADCs cytotoxin

－

－

－

IC50

－

－

－

－

－

體外研究

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.

體內(nèi)研究

N/A

臨床實(shí)驗(yàn)

N/A

特征

N/A

酶活性檢測實(shí)驗(yàn)

方法

N/A

細(xì)胞實(shí)驗(yàn)

細(xì)胞系

N/A

濃度

N/A

處理時(shí)間

N/A

方法

N/A

動物實(shí)驗(yàn)

動物模型

N/A

配制

N/A

劑量

N/A

給藥方式

N/A

產(chǎn)品編號

產(chǎn)品名稱

包裝

KL2243-10mM

MMAF (Tubulin抑制劑)

10mM×0.2ml

KL2243-5mg

MMAF (Tubulin抑制劑)

5mg

KL243-25mg

MMAF (Tubulin抑制劑)

25mg

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說明書

1份