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Pertuzumab, a humanized IgG1 monoclonal antibody, is a HER2 dimerization inhibitor for the treatment of metastatic HER2-positive breast cancer.

For research use only. We do not sell to patients.

Pertuzumab Chemical Structure

Pertuzumab Chemical Structure

CAS No. : 380610-27-5

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Based on 3 publication(s) in Google Scholar

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Description

Pertuzumab, a humanized IgG1 monoclonal antibody, is a HER2 dimerization inhibitor for the treatment of metastatic HER2-positive breast cancer.

IC50 & Target

HER2

 

In Vitro

Trastuzumab and Pertuzumab are highly synergistic inhibitors of BT474 breast cancer cell survival. The combination of trastuzumab and Pertuzumab mediates a loss of up to 60% of cells at doses in which individual drugs do not alter cell survival. The combination of trastuzumab and Pertuzumab reduces the percentage of proliferating (S-phase) cells by more than 2-fold. A combination of trastuzumab and Pertuzumab inhibits cell proliferation and survival to a greater degree than does either agent alone[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

In Calu-3 NSCLC xenografts, monotherapy with pertuzumab or trastuzumab is able to significantly inhibit tumor growth, with treatment-to-control ratios (TCR) of 0.23 and 0.27, respectively. The combination of trastuzumab and pertuzumab produces a dramatically enhanced antitumor activity compared with single-agent treatments (TCR 0.05, resulting in tumor regression and, in 3 of 10 animals, complete tumor remission). Treatment of KPL-4 breast cancer xenografts with either trastuzumab or pertuzumab inhibits tumor growth with TCRs of 0.67 and 0.65, respectively. Pertuzumab maintains antitumor activity after progression on trastuzumab[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

145175.18

CAS No.
Appearance

Liquid

Color

Colorless to light yellow

SMILES

[Pertuzumab]

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Purity: 99.80%

References
Cell Assay
[1]

BT474 cells are seeded at 5×104 cells/well in 12-well dishes. After 24 h, cells are treated in triplicate with 2-fold serial dilutions of trastuzumab, Pertuzumab, or both drugs simultaneously at a fixed 1:1 ratio at low doses ranging from 0.9 ng/mL to 10 ng/mL. After 5 days, cells are trypsinized and counted by trypan blue exclusion. Growth inhibition is calculated as the percentage of viable cells compared with untreated cultures[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

Mice: Calu-3 or KPL-4 tumors (100 mm3) are treated with trastuzumab (30 mg/kg loading dose, then 15 mg/kg weekly), Pertuzumab (30 mg/kg loading dose, then 15 mg/kg weekly), or both, administered i.p. for the duration of the study. Tumor volumes and body weights are measured twice weekly. For the acute study, advanced Calu-3 tumors of 400 mm3 are treated once with trastuzumab and/or Pertuzumab at a dose of 30 mg/kg. Samples are harvested 7 d later for immunohistochemistry (IHC) and Western blot analysis[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Pertuzumab Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Pertuzumab
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