化学信息:
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。 |
生物信息:
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 | - | - | - |
IC50 | - | - | - | - | - |
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 |
相关实验数据(此数据来自于公开文献,碧云天并不保证其有效性):
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 |
SC2243-10mM | MMAF (Tubulin抑制剂) | 10mM×0.2ml |
SC2243-5mg | MMAF (Tubulin抑制剂) | 5mg |
SC2243-25mg | MMAF (Tubulin抑制剂) | 25mg |
— | 说明书 | 1份 |
保存条件:
-20℃保存,至少一年有效。5mg和25mg包装也可室温保存,至少6个月有效。如果溶于非DMSO溶剂,建议分装后-80℃保存,预计6个月内有效。