Pertuzumab

Catalog No.A2008 Synonyms: Omnitarg, 2C4 Non-humanized mouse model applicable

For research use only. Not for use in humans.

Pertuzumab, a humanized monoclonal antibody and the first in the class of agents called the HER2 dimerization inhibitors, impairs the ability of HER2 to bind to other members of the HER family, MW: 148 KD.

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Biological Activity

Description Pertuzumab, a humanized monoclonal antibody and the first in the class of agents called the HER2 dimerization inhibitors, impairs the ability of HER2 to bind to other members of the HER family, MW: 148 KD.
Targets
HER2 [1]
()
In vitro

Pertuzumab significantly inhibits the HRG-α-stimulated cellular growth of the 11_18 cells. Pertuzumab blocks HRG-α-stimulated phosphorylation of HER3, mitogen-activated protein kinase (MAPK), and Akt. In contrast, pertuzumab fails to block epidermal growth factor (EGF)-stimulated phosphorylation of EGF receptor (EGFR) and MAPK. Immunoprecipitation shows that pertuzumab inhibited HRG-α-stimulated HER2/HER3 heterodimer formation. HRG-α-stimulated HER3 phosphorylation is also observed in the PC-9 cells co-overexpressing EGFR, HER2, and HER3, but the cell growth is neither stimulated by HRG-α nor inhibited by pertuzumab[1]. Pertuzumab binds to ErbB2 near the center of domain II, sterically blocking a binding pocket necessary for receptor dimerization and signaling. Pertuzumab is specific for human ErbB2 and does not bind to rodent ErbB2 (neu) with detectable affinity[1].

In vivo Pertuzumab has antitumor activity as a single agent in a mouse xenograft model and the combination with trastuzumab strongly reduces EGFR-HER2 signaling and shows significant antitumor activity compared with each monotherapy in NCI-N87, an HER2-positive human gastric cancer xenograft model[3].

Protocol

Cell Research:
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  • Objective: Growth inhibition assay
    Cells: Human lung cancer cell lines (11_18 cells and Ma-24 cells)
    Concentrations: 0.01, 0.1, 1, 10, 100μg/mL
    Incubation Time: 72 h
    Method: The lung cells are exposed to pertuzumab (0.01-100 μg/mL) for 72 h in serum free medium with or without 100 ng/mL of epidermal growth factor (EGF), transforming growth factor (TGF)-α, heparin-binding epidermal growth factor (HB-EGF), orheregulin (HRG)-α. The viability is determined using the MTS assay.
    Reference: https://www.ncbi.nlm.nih.gov/pubmed/17627612

    Objective: Antibody-dependent cellular cytotoxicity (ADCC)
    Cells: peripheral blood lymphocytes (PBLs), USPC cell lines (Uterine cancer cell)
    Concentrations: 2.5 μg/mL
    Incubation Time: --
    Method: A standard 5 h chromium (51Cr) release assay was performed to measure the cytotoxic reactivity of peripheral blood lymphocytes (PBLs) from several healthy donors in combination with trastuzumab and/or pertuzumab against USPC target cell lines.
    Reference: https://www.ncbi.nlm.nih.gov/pubmed/19920829

    Pertuzumab can apply to nude mice, various cancer cell lines and other related assays (Only for Reference)
Animal Research:
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  • Objective: In vivo tumor growth inhibition studies
    Animal Models: BALB-nu/nu mice
    Formulation: saline
    Dosages: 20 mg/kg, 40 mg/kg and 80 mg/kg
    Administration: i.p.
    Reference: https://www.ncbi.nlm.nih.gov/pubmed/21700765

    Objective: To investigate the antitumor activity of the combination of pertuzumab and trastuzumab for gastric cancer
    Animal Models: BALB-nu/nu mice were inoculated subcutaneously with human gastric cancer cell lines MKN-28 or NCI-N87, or an 8-mm3 piece of 4-1ST tumor tissue
    Formulation: saline
    Dosages: 20 mg/kg, 40 mg/kg and 80 mg/kg
    Administration: i.p.
    Reference: https://www.ncbi.nlm.nih.gov/pubmed/21700765

    Ttrastuzumab can apply to immunodeficient mice (eg: SCID mice), various cancer cell lines and other related assays (Only for Reference)

Product Details

Formulation PBS buffer, pH 7.2
Isotype Human IgG
Source CHO cells
Storage Store at -80°C and avoid freeze-thaw cycles.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID