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一甲基澳瑞他汀 E /Monomethyl auristatin E {[allProObj[0].p_purity_real_show]}

货号:A172961 同义名: MMAE;Vedotin

Monomethyl auristatin E(MMAE;SGD-1010)是杜氏素10的合成衍生物,通过抑制微管蛋白聚合而起到强效有丝分裂抑制剂的作用。MMAE广泛用于抗体-药物结合物(ADC)的细胞毒性成分,以治疗各种癌症。

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Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
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Monomethyl auristatin E 化学结构 CAS号:474645-27-7
Monomethyl auristatin E 化学结构
CAS号:474645-27-7
Monomethyl auristatin E 3D分子结构
CAS号:474645-27-7
Monomethyl auristatin E 化学结构 CAS号:474645-27-7
Monomethyl auristatin E 3D分子结构 CAS号:474645-27-7
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Monomethyl auristatin E 纯度/质量文件 产品仅供科研

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Monomethyl auristatin E 生物活性

描述 Monomethyl auristatin E (MMAE) produced under Good Manufacturing Practice (GMP) guidelines is a version of MMAE that inhibits tubulin polymerization[1].
体内研究

The combination of Monomethyl auristatin E (MMAE) with ionizing radiation (IR) leads to delayed tumor growth, whereas the use of tumor-targeting ACPP-cRGD-MMAE alongside IR results in a more pronounced and prolonged regression of tumors in xenograft models[2].

体外研究

Within CD30+ cancer cells, Monomethyl auristatin E (MMAE) is effectively liberated from SGN-35 and can kill adjacent non-targeted cells due to its ability to permeate cell membranes[1].

MMAE enhances the sensitivity of colorectal and pancreatic cancer cells to ionizing radiation (IR) in a manner that is both schedule and dose-dependent, which is associated with mitotic arrest. This increased radiosensitivity results in reduced clonogenic survival and a higher incidence of DNA double-strand breaks in cells subjected to irradiation[2].

作用机制 MMAE binds to tubulin and interferes with microtubule formation.[4]

Monomethyl auristatin E 动物研究

Dose Cynomolgus monkey: 0.3 mg/kg - 3 mg/kg[5] (i.v.) Rat: 0.03 mg/kg - 0.2 mg/kg[6] (i.v.) Mice: 0.3 mg/kg[7] (i.v.)
Administration i.v.

Monomethyl auristatin E 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02227199 Recurrent Adult Hodgkin Lympho... 展开 >>ma Refractory Hodgkin Lymphoma TNFRSF8 Positive 收起 << Phase 1 Phase 2 Recruiting - United States, Washington ... 展开 >> Fred Hutch/University of Washington Cancer Consortium Recruiting Seattle, Washington, United States, 98109 Contact: Ajay K. Gopal    206-606-2037    agopal@u.washington.edu    Principal Investigator: Ajay K. Gopal 收起 <<
NCT00866047 - Completed - -
NCT02001623 Ovary Cancer ... 展开 >>Cervix Cancer Endometrium Cancer Bladder Cancer Prostate Cancer (CRPC) Esophagus Cancer Lung Cancer(NSCLC) Squamous Cell Carcinoma of the Head and Neck (SCCHN) 收起 << Phase 1 Phase 2 Active, not recruiting December 2018 -

Monomethyl auristatin E 参考文献

[1]Yang SY, Li LL. The purposes of 5H- [1,2,4] triazine [5,6-b] indole derivatives of 3 substitutions. CN108309982A. 2017.

[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.

Monomethyl auristatin E 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.39mL

0.28mL

0.14mL

6.96mL

1.39mL

0.70mL

13.93mL

2.79mL

1.39mL

Monomethyl auristatin E 技术信息

CAS号474645-27-7
分子式C39H67N5O7
分子量 717.979
别名 MMAE;Vedotin;Brentuximab vedotin;SGD-1010
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Sealed in dry,2-8°C

溶解度

DMSO: 50 mg/mL(69.64 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

无水乙醇: 45 mg/mL(62.68 mM),配合低频超声助溶,注意:无水乙醇开封后,易挥发,也会吸收空气中的水分,导致溶解能力下降,请避免使用开封较久的乙醇

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