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Pertuzumab (also known as 2C4; trade name Perjeta) is a humanized monoclonal antibody that acts as a HER2 dimerization inhibitor for the treatment of metastatic HER2-positive breast cancer. Pertuzumab is used in combination with trastuzumab and docetaxel for the treatment of metastatic HER2-positive breast cancer; it also used in the same combination as a neoadjuvant in early HER2-positive breast cancer
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The extremely synergistic inhibitors of BT474 breast cancer cell survival are trastuzumab and pertuzumab. When trastuzumab and pertuzumab are used together, cell survival is not affected by either treatment alone, but up to 60% of cells can be lost. Trastuzumab with Pertuzumab together more than double the percentage of proliferating (S-phase) cells. Cell survival and proliferation are more severely inhibited by trastuzumab and pertuzumab together than by either drug alone[1].
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| ln Vivo |
Treatment-to-control ratios (TCR) of 0.23 and 0.27, respectively, indicate that monotherapy with pertuzumab or trastuzumab can significantly reduce tumor growth in Calu-3 NSCLC xenografts. When trastuzumab and pertuzumab are used together, the anticancer activity is significantly increased as compared to single-agent therapies (TCR 0.05), leading to tumor regression and, in three out of ten mice, total tumor remission. Tumor growth is inhibited in KPL-4 breast cancer xenografts treated with trastuzumab or pertuzumab, with TCRs of 0.67 and 0.65, respectively. Following trastuzumab progression, pertuzumab continues to have anticancer activity[2].
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| References |
[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.
[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 |
| CAS # |
380610-27-5
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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