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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. |
| Related EGFR/HER2 Products |
|---|
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| HKI-357
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| SJF-1528
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| CH7233163
CH7233163 is a noncovalent ATP-competitive inhibitor for EGFR-Del19/T790M/C797S. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
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