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  • 產(chǎn)品名稱(chēng): VcMMAE
  • 產(chǎn)品貨號(hào): CS00443
  • 貨期: 現(xiàn)貨
  • 價(jià)格與訂購(gòu): 240
  • 數(shù)量:
    庫(kù)存: 10
  • 規(guī)格: 1mg
  • 產(chǎn)品信息
  • 如何訂購(gòu)
    產(chǎn)品描述
    VcMMAE is a drug-linker conjugate for ADC with potent antitumor activity. 
    靶點(diǎn)活性
    Microtubule/Tubulin
    體外活性
    MMAE sensitized colorectal and pancreatic cancer cells to IR in a schedule and dose dependent manner correlating with mitotic arrest. 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. Radiosensitization is evidenced by decreased clonogenic survival and increased DNA double strand breaks in irradiated cells. 
    體內(nèi)活性
    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 prolonged tumor regression in xenograft models. 
    動(dòng)物實(shí)驗(yàn)
    6-8 week old female athymic nu/nu mice are injected subcutaneously into thighs with 5×106 HCT-116 or PANC-1 cells in a 1:1 Matrigel and PBS solution. Mice are treated with IR or intravenous (IV) injection of ACPP-cRGD-MMAE (6 nmoles/day, 18 nmoles total, i.v.), tumor tissue is harvested, formalin fixed and paraffin embedded followed by staining with indicated antibodies. The primary antibody is used at a 1:250 dilution and is visualized using DAB as a chromagen with the UltraMap system. 
    細(xì)胞實(shí)驗(yàn)
    Monomethyl auristatin E is reconstituted in DMSO at a concentration of 5 nM. Monomethyl auristatin E (MMAE, 5 nM) and ionizing radiation (IR) treated cells are harvested and lysed in RIPA buffer with protease and phosphatase inhibitors. 30 μg of lysate undergo electrophoresis using 4-12% Bis-Tris gels, transferred to PVDF membranes and incubated with indicated primary antibodies. 
    別名
     mc-vc-PAB-MMAE , 化合物VCMMAE mc-vc-PAB-MMAE 
    純度
    98%
    分子量
    1316.65
    分子式
    C68H105N11O15 
    CAS No.
    646502-53-6 
    存儲(chǔ)
    Powder: -20°C for 3 years
    In solvent: -80°C for 2 years
    溶解度
    DMSO: 54 mg/mL, VcmMAE is dissolved in DMSO and then diluted with 0.9% NaCl
    ( < 1 mg/ml refers to the product slightly soluble or insoluble )
    參考文獻(xiàn)
    1. Okeley, et al. Intracellular Activation of SGN-35, a Potent Anti-CD30 Antibody-Drug Conjugate. Clinicalal 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.
    4. Jianmin Fang, et al. Anti-her2 antibody and conjugate thereof. US 20160304621 A1.
    Note
    For research use only .
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