Monomethyl auristatin E (Synonyms: MMAE; SGD-1010; Vedotin)
目录号: PL04365 纯度: ≥99%
CAS No. :474645-27-7
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中文名称
Monomethyl auristatin E
中文别名
Monomethyl auristatin E (MMAE) 抑制剂;一甲基澳瑞他汀E;Microtubule抑制剂;Monomethyl auristatin E (MMAE);Monomethyl auristatin E
英文名称
Monomethyl auristatin E
英文别名
Monomethyl auristatin E (MMAE);(S)-N-((3R,4S,5S)-1-((S)-2-((1R,2R)-3-(((1R,2R)-1-Hydroxy-1-phenylpropan-2-yl)amino)-1-methoxy-2-methyl-3-oxopropyl)pyrrolidin-1-yl)-3-methoxy-5-methyl-1-oxohe;[3H]-Vedotin;MMAE;MMAE(Monomethyl Auristain E);MONOMETHYL AURISTATIN E;Vedotin;N-Methyl-L-valyl-N-[(1S,2R)-4-[(2S)-2-[(1R,2R)-3-[[(1R,2S)-2-hydroxy-1-methyl-2-phenylethyl]amino]-1-methoxy-2-methyl-3-oxopropyl]-1-pyrrolidinyl]-2-methoxy-1-[(1S)-1-methylpropyl]-4-oxobutyl]-N-methyl-L-valinamide;(S)-N-((3R,4S,5S)-1-((S)-2-((1R,2R)-3-(((1R,2R)-1-hydroxy-1-phenylpropan-2-yl)amino)-1-methoxy-2-methyl-3-oxopropyl)pyrrolidin-1-yl)-3-methoxy-5-methyl-1-oxoheptan-4-yl)-N,3-dimethyl-2-((S)-3-methyl-2-(methylamino)butanamido)butanamide;(2S)-N-[(2S)-1-[[(3R,4S,5S)-1-[(2S)-2-[(1R,2R)-3-[[(1R,2R)-1-Hydroxy-1-phenylpropan-2-yl]amino]-1-me
Cas No.
474645-27-7
分子式
C39H67N5O7
分子量
717.98
包装储存
-20°C, sealed storage, away from moisture and light 该产品在溶液状态不稳定,建议您现用现配,即刻使用。
产品详情
Monomethyl auristatin E (MMAE; SGD-1010) 是海兔毒素 10 的合成衍生物,通过抑制微管蛋白聚合而起到有效的有丝分裂抑制作用。 MMAE 广泛用作细胞毒性成分制作抗体偶联药物 (ADCs) 用于癌症的研究。
生物活性
Monomethyl auristatin E (MMAE; SGD-1010) is a synthetic derivative of dolastatin 10 and functions as a potent mitotic inhibitor by inhibiting tubulin polymerization. MMAE is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) to treat several different cancer types.
性状
Solid
IC50 & Target[1][2]
Auristatin
体外研究(In Vitro)
Monomethyl auristatin E (MMAE) is efficiently released from SGN-35 within CD30 cancer cells and, due to its membrane permeability, is able to exert cytotoxic activity on bystander cells. MMAE sensitizes colorectal and pancreatic cancer cells to IR in a schedule and dose dependent manner correlating with mitotic arrest. Radiosensitization is evidenced by decreased clonogenic survival and increased DNA double strand breaks in irradiated cells. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Monomethyl auristatin E (MMAE) in combination with IR results in tumor growth delay, tumor-targeted ACPP-cRGD-MMAE with IR produces a more robust and significantly prolongs tumor regression in xenograft models. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-20°C, sealed storage, away from moisture and light 该产品在溶液状态不稳定,建议您现用现配,即刻使用。
ClinicalTrial
参考文献
[1]. Okeley, et al. Intracellular Activation of SGN-35, a Potent Anti-CD30 Antibody-Drug Conjugate. Clinical Cancer Research (2010), 16(3), 888-897.
[2]. Lisa Buckel, et al. Tumor radiosensitization by monomethyl auristatin E: mechanism of action and targeted delivery. Cancer Res. 2015 Apr 1;75(7):1376-87.
溶解度数据
In Vitro: Ethanol : 50 mg/mL (69.64 mM; Need ultrasonic)DMSO : ≥ 48 mg/mL (66.85 mM)
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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