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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. 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.
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.
NPJ Breast Cancer. 2022 Jan;8(1):1.
Effects of neoadjuvant trastuzumab, pertuzumab and palbociclib on Ki67 in HER2 and ER-positive breast cancer
Pertuzumab purchased from AbMole
| Cell Experiment | |
|---|---|
| Cell lines | The lung cells (11_18 cells and Ma-24 cells) |
| Preparation 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. |
| Concentrations | 0.01-100 μg/mL |
| Incubation time | 72 h |
| Animal Experiment | |
|---|---|
| Animal models | BALB-nu/nu mice |
| Formulation | saline |
| Dosages | 20 mg/kg, 40 mg/kg and 80 mg/kg |
| Administration | i.p. |
| Molecular Weight | 145175.18 |
| CAS Number | 380610-27-5 |
| Storage | Store at -20°C or -70°C. Avoid multiple freeze-thaws. |
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