Pertuzumab (Anti-Human HER2, Humanized Antibody) |
| Catalog No.GC34210 |
Pertuzumab (Anti-Human HER2, Humanized Antibody), the first of a new class of agents designated as HER dimerisation inhibitors, is a humanised IgG1 monoclonal antibody (mAb) that sterically binds domain II of the erbB2 receptor.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 380610-27-5
Sample solution is provided at 25 µL, 10mM.
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Pertuzumab (Anti-Human HER2, Humanized Antibody), the first of a new class of agents designated as HER dimerisation inhibitors, is a humanised IgG1 monoclonal antibody (mAb) that sterically binds domain II of the erbB2 receptor [1].
Pertuzumab may mostly act to inhibit the classical signaling pathways stimulated by active HER2, including receptor dimerization, receptor phosphorylation and the activation of signaling proteins downstream from HER receptors, including Erk and Akt [2].
Pertuzumab was approved by the FDA in 2012 to be used in combination with trastuzumab and docetaxel for treating metastatic breast cancer patients [2]. In humans, pooled analysis from one phase IA and two phase II studies in advanced disease evaluated pertuzumab pharmacokinetic parameters demonstrated minor interpatient variability in clearance and volume distribution when pertuzumab was administered with a fixed dose or based on weight (mg/kg). This supports the use of fixed dosing of pertuzumab, with an initial loading dose (840 mg) followed by a fixed dose of 420 mg every 3 weeks [3].
References:
[1]. K El-Sahwi, S Bellone, E Cocco, et al. In vitro activity of pertuzumab in combination with trastuzumab in uterine serous papillary adenocarcinoma. Br J Cancer, 102 (2010), pp. 134-143
[2]. Nami B, Maadi H, Wang Z. Mechanisms underlying the action and synergism of trastuzumab and pertuzumab in targeting HER2-positive breast cancer. Cancers (Basel) 2018;10
[3]. Capelan, M. et al. Pertuzumab: new hope for patients with HER2-positive breast cancer. Ann. Oncol. 24, 273-282 (2013).
| Cell experiment [1]: | |
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Cell lines |
Primary USPC cells |
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Preparation Method |
Primary USPC cells were seeded in a 96-well plate at a density of 2000-5000 cells per well in RPMI 1640 medium with 10% foetal bovine serum. After 24 h, pertuzumab, trastuzumab, and a 1 : 1 combination of both antibodies were added at a final concentration of 20 µg ml-1. The final volume of medium per well was set at 100 µl for 48-72 h |
|
Reaction Conditions |
20 µg ml-1 for 48-72 hours |
|
Applications |
Cell proliferation was significantly inhibited in the presence of pertuzumab, trastuzumab, and the combination of the two mAbs in all USPC cell lines tested, with the percentage of inhibition varying from 4 to 59% (pertuzumab), 3 to 48% (trastuzumab), and 7 to 63% (mAbs combination) in multiple experiments. |
| Animal experiment [2]: | |
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Animal models |
Male CD-1 mice |
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Preparation Method |
Pertuzumab (26.7 mg/mL) and vehicle (10 mM L-histidine at pH 6.0, 240 mM sucrose, 0.02% polysorbate 20) were stored at 2-8℃. |
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Dosage form |
3, 30, or 90 mg/kg, intravenous (IV) bolus. |
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Applications |
The distribution phase of pertuzumab was <1 day, the terminal elimination half-life was approximately 10 days, and the volume of distribution was 27–58 mL/kg. |
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References: [1]: K El-Sahwi, S Bellone, E Cocco, et al. In vitro activity of pertuzumab in combination with trastuzumab in uterine serous papillary adenocarcinoma. Br J Cancer, 102 (2010), pp. 134-143 |
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| Cas No. | 380610-27-5 | SDF | |
| Canonical SMILES | [Pertuzumab] | ||
| Formula | M.Wt | 145175.18 | |
| Solubility | Soluble in water | Storage | Store at -80°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.0069 mL | 0.0344 mL | 0.0689 mL |
| 5 mM | 0.0014 mL | 0.0069 mL | 0.0138 mL |
| 10 mM | 0.0007 mL | 0.0034 mL | 0.0069 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
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