Pertuzumab 

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

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 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.

380610-27-5

Liquid

Colorless to light yellow

[Pertuzumab]

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

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  Human IgG1 kappa

• 
  Immobilized HER2/CD340 Protein, Human can bind Pertuzumab. The EC₅₀ for this effect is 42.59 ng/mL.
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  Pertuzumab has a significant ADCC effect on SK-BR-3 cells in a dose-dependent manner.The EC₅₀ for this effect is 61.54 and 74.56 ng/mL.

• [1]. Nahta R, et al. The HER-2-targeting antibodies trastuzumab and pertuzumab synergistically inhibit the survivalof breast cancer cells. Cancer Res. 2004 Apr 1;64(7):2343-6.  [Content Brief]

  [2]. Scheuer W, et al. Strongly enhanced antitumor activity of trastuzumab and pertuzumab combination treatment on HER2-positive human xenograft tumor models. Cancer Res. 2009 Dec 15;69(24):9330-6.  [Content Brief]