1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEMonomethyl auristatin ECat. No.: HY-15162CAS No.: 474645-27-7Synonyms: MMAE; SGD-1010分式: CHNO分量: 717.98作靶點: Microtubule/Tubulin; ADC Cytotoxin作通路: Cell Cycle/DNA Damage; Cytoskeleton; Antibody-drugConjugate/ADC Related儲存式: 4C, s

2、tored under nitrogen* In solvent : -80C, 6 months; -20C, 1 month (stored undernitrogen)溶解性數(shù)據(jù)體外實驗 DMSO : 48 mg/mL (66.85 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 1.3928 mL 6.9640 mL 13.9280 mL5 mM 0.2786 mL 1.3928 mL 2.7856 mL10 mM 0.1393 mL 0.6964

3、 mL 1.3928 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Monomethyl auristatin E (MMAE; SGD-1010)海兔毒素10的合成衍物，通過抑制微管蛋聚合起到有效的有絲分裂抑制作。 MMAE泛作細胞毒性成分制作抗體-藥物偶聯(lián)物 (ADCs) 以治療癌癥。IC50 & Target Microtubule 11/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE體外研究 Monomethyl auristatin E (MMA

4、E) is efficiently released from SGN-35 within CD30+ cancer cells and, due toits membrane permeability, is able to exert cytotoxic activity on bystander cells 1. MMAE sensitizescolorectal and pancreatic cancer cells to IR in a schedule and dose dependent manner correlating withmitotic arrest. Radiose

5、nsitization is evidenced by decreased clonogenic survival and increased DNA doublestrand breaks in irradiated cells 2.體內(nèi)研究 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 tumo

6、r regression in xenograftmodels 2.PROTOCOLCell Assay 2 Monomethyl auristatin E (MMAE, 5 nM) and ionizing radiation (IR) treated cells are harvested and lysed inRIPA buffer with protease and phosphatase inhibitors. Thirty g of lysate undergo electrophoresis using 4-12% Bis-Tris gels, transferred to P

7、VDF membranes and incubated with indicated primary antibodies. Blotsare developed by ECL.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice 2Administration 2 6-8 week old female athymic nu/nu mice are injected subcutaneously into thighs with 51

8、06 HCT-116 orPANC-1 cells in a 1:1 Matrigel and PBS solution. Mice are treated with IR or intravenous (IV) injection ofACPP-cRGD-MMAE (6 nmoles/day, 18 nmoles total, i.v.), tumor tissue is harvested, formalin fixed andparaffin embedded followed by staining with indicated antibodies. The primary anti

9、body is used at a 1:250dilution and is visualized using DAB as a chromagen with the UltraMap system.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻 Mol Ther Nucleic Acids. 2018 Mar 2;10:227-236. Int J Cancer. 2015 Sep;137(6):1457-66. Mol Pha

10、rm. 2019 Jun. ACS Chem Biol. 2018 Mar 16;13(3):761-771. Sci Rep. 2018 Sep 21;8(1):14211.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. 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. 2015Apr 1;75(7):1376-87.McePdfHeight2/2 Master of Small Molecules 您邊的抑制劑師www.MedChemECaution: Product has not been