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Trastuzumab

Cat. No. M6218
Trastuzumab Structure
Synonym:

Herceptin

Size Price Availability Quantity
1mg USD 200  USD200 In stock
5mg USD 600  USD600 In stock
10mg USD 900  USD900 In stock
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Quality Control & Documentation
Biological Activity

In vitro: Trastuzumab has been demonstrated to exert a variety of anti-tumor effects selectively in HER2-overexpressing tumor cells. Trastuzumab binds to the juxtamembrane domain of HER2 and upon receptor binding, the antibody downregulates the expression of HER2. Trastuzumab selectively blocks ligand-independent HER2-HER3 dimerization. In addition, trastuzumab binding to HER2 blocks proteolytic cleavage of the extracellular domain of HER2, resulting in diminished levels of the more active p95-HER2 form of HER2. As a result of these effects on the HER2 receptor, trastuzumab causes downregulation of PI3K pathway signaling and downstream mediators of cell cycle progression such as cyclin D1. Trastuzumab not only inhibits HER2 signaling pathways but also triggers immune-mediated responses against HER2-overexpressing cells. Trastuzumab binding engages Fc receptors on immune effector cells leading to antibody-dependent cellular cytotoxicity. Beyond these effects, trastuzumab has been shown to have antiangiogenic effects and to lower the proapoptotic threshold for chemotherapy.

In vivo: Trastuzumab is shown to be safe when administered chronically to a range of animals including primates. In experiments mimicking adjuvant therapy of submacroscopic disease in vivo (JIMT-1 cells inoculated s.c. in severe combined immunodeficiency mice), trastuzumab is able to inhibit the outgrowth of macroscopically detectable xenograft tumors for up to 5-7 weeks. Trastuzumab has a remarkable antitumor effect and is currently used worldwide for the treatment of breast cancer. In in vivo models, trastuzumab decreases the microvessel density of breast cancer xenografts. It is well documented that trastuzumab acts directly in cancer cell signaling, as well as indirectly via the immune system.

Product Citations
Protocol (for reference only)
Cell Experiment
Cell lines JIMT-1, SKBR-3, and BT-474 cells
Preparation method Exponentially growing cells are harvested and plated in single wells of a 96-well flat-bottomed tissue culture plate at defined densities, ranging from 4,500–8,000 cells per well depending on the cell line. After overnight culture, the regular medium is exchanged to medium containing 0, 1, 10, or 100 μg/mL trastuzumab or trastuzumab-F(ab′)2. Cell viability is tested after 72 h of treatment. Fluorescence is detected at an excitation of 544 nm, and emission is detected at 590 nm.
Concentrations 0, 1, 10, or 100 μg/mL
Incubation time 72 h
Animal Experiment
Animal models SCID C.B-17 scid/scid and nu/nmri nude mouse
Formulation saline
Dosages 5 μg/g
Administration i.p.
Chemical Information
Molecular Weight 145529.41
Formula C6470H10012N1726O2013S42
CAS Number 180288-69-1
Storage Store at -20°C or -70°C. Avoid multiple freeze-thaws.
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Okita R, et al. Oncol Rep. Lapatinib enhances trastuzumab-mediated antibody-dependent cellular cytotoxicity via upregulation of HER2 in malignant mesothelioma cells.

[2] Han X, et al. Oncotarget. Tunicamycin enhances the antitumor activity of trastuzumab on breast cancer in vitro and in vivo.

[3] Hiroshima Y, et al. PLoS One. Tumor-Targeting Salmonella typhimurium A1-R in Combination with Trastuzumab Eradicates HER-2-Positive Cervical Cancer Cells in Pat ient-Derived Mouse Models.

[4] Nahta R, et al. Oncogene. Trastuzumab: triumphs and tribulations.

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Keywords: Trastuzumab, Herceptin supplier, EGFR/HER2, inhibitors, activators


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