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Applications: Study enzyme kinetics and screen small molecule inhibitors for drug discovery and high throughput screening (HTS) applications.
Background: HER2 (human epidermal growth factor receptor 2), also known as erbB-2 or CD340, is a tyrosine kinase of the EFGR family of proteins. There is no known ligand, but it can form homodimers or heterodimers with other HER proteins. Once active, it activates the MAPK (mitogen-activated protein kinase) and PI3K (phosphatidylinositol-3 kinase) signaling pathways resulting in cell cycle progression and cell proliferation. HER2 over-expression is also known to occur in breast, ovarian, stomach, lung adenocarcinoma, aggressive forms of uterine cancer and gastric cancer. In 1990 the FDA approved the use of the monoclonal antibody trastuzumab in breast and stomach cancer. Other strategies to target HER2 that have been approved include ADCs (antibody-drug conjugate) and margetuximab (an HER2 antibody that can alter the Fc-receptor affinity to CD16 and induce cytotoxicity). The use of small molecule tyrosine kinase inhibitors, alone or in combinatory therapy, has shown great promise in the treatment of HER2+ breast cancer (BC). However, resistance to treatment, for instance by mutations on HER2 or upregulation of other HER receptors, has been described. Neratinib, a pan-HER2 inhibitor, was approved in 2017 for early-stage BC, as adjuvant anti-HER2 therapy after trastuzumab treatment. However, side effects limit its use. The development of treatments able to target early-stage cancer, with minimal side effects and resistance development, will bring major benefits to HER2+ oncology patients.
Contraindications: The final concentration of DMSO in the assay should not exceed 1%.
Description: The Chemi-Verse™ HER2 Kinase Assay Kit is designed to measure HER2 (human epidermal growth factor receptor 2) tyrosine kinase activity for screening and profiling applications using ADP-Glo™ as a detection reagent. The assay kit comes in a convenient 96-well format, with enough purified HER2 (amino acids 679-1255), kinase substrate, ATP, and kinase assay buffer for 100 enzyme reactions.
Storage Stability: This assay kit will perform optimally for up to 6 months from date of receipt when the materials are stored as directed.
Uniprot: P04626
Warnings: Avoid freeze/thaw cycles
Biosafety Level: Not applicable (BSL-1)
References: Schlam I. and Swain S., 2021 npj Breast Cancer 7: 56.
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