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Pertuzumab

Cat. No. M6221
Pertuzumab Structure
Synonym:

Omnitarg, 2C4

Size Price Availability Quantity
5mg USD 800 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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.

Protocol
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.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight
Formula
CAS Number
Purity >98%
Solubility
Storage at -20°C
References

miRNA-150 downregulation promotes pertuzumab resistance in ovarian cancer cells via AKT activation.
Wuerkenbieke D, et al. Arch Gynecol Obstet. 2015 Nov;292(5):1109-16. PMID: 25986891.

Pertuzumab, trastuzumab, and docetaxel in HER2-positive metastatic breast cancer.
Swain SM, et al. N Engl J Med. 2015 Feb 19;372(8):724-34. PMID: 25693012.

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Keywords: Pertuzumab, Omnitarg, 2C4 supplier, EGFR/HER2, inhibitors

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