33-047
PI 3-Kinase 3-step HTRF® Assay
The PI 3-Kinase 3-Step HTRF Assay is a high-performance assay kit that provides a universal method for testing all Class I PI3-Kinases in a homogeneous format.
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UNSPSC Code:
12161503
eCl@ss:
32161000
NACRES:
NA.84
Recommended Products
Quality Level
species reactivity
human, mouse
manufacturer/tradename
HTRF®
Upstate®
technique(s)
activity assay: suitable (kinase)
NCBI accession no.
UniProt accession no.
detection method
fluorometric (HTRF)
shipped in
dry ice
Gene Information
human ... PIK3CA(5290)
General description
Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit α (PIK3CA) gene is mapped to human chromosome 3q26.32. This gene codes for the catalytic subunit p110α of class IA PI3-kinase. PI3K signaling pathways regulate various cellular activities and properties including proliferation, survival, apoptosis, motility, and morphology. Mutation or overexpression of the PIK3CA gene is implicated in the development of various human solid tumors including head and neck cancers or pharyngeal cancer and ovarian cancer.
Application
PI 3-Kinase 3-step HTRF® Assay has been used to determine the in vitro inhibitory potencies of phosphatidylinositol 3-kinase (PI3K) δ inhibitors such as MSD-496486311, MSD126796721, idelalisib, and duvelisib across PI3K α, β, γ, and δ isoforms.
Biochem/physiol Actions
Target Sub-Family: PI3K/PI4K
Packaging
Kit capacity: 10,000 wells
Components
4X Reaction Buffer
PIP2 (substrate, 1mM stock)
DM A Reaction Buffer
DM B Reaction Buffer
DM C Reaction Buffer
BPIP3
Stop Reagent
PIP2 (substrate, 1mM stock)
DM A Reaction Buffer
DM B Reaction Buffer
DM C Reaction Buffer
BPIP3
Stop Reagent
Storage and Stability
12 months at -70°C
Other Notes
Research Category
Apoptosis & Cancer
Research Sub Category
Oncology
Apoptosis & Cancer
Research Sub Category
Oncology
Legal Information
HTRF is a registered trademark of Cis Bio International
UPSTATE is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Unless otherwise stated in our catalog or other company documentation accompanying the product(s), our products are intended for research use only and are not to be used for any other purpose, which includes but is not limited to, unauthorized commercial uses, in vitro diagnostic uses, ex vivo or in vivo therapeutic uses or any type of consumption or application to humans or animals.
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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Andreas G Bader et al.
Nature reviews. Cancer, 5(12), 921-929 (2005-12-13)
There have long been indications of a role for PI3K (phosphatidylinositol 3-kinase) in cancer pathogenesis. Experimental data document a requirement for deregulation of both transcription and translation in PI3K-mediated oncogenic transformation. The recent discoveries of cancer-specific mutations in PIK3CA, the
Robbie L McLeod et al.
The Journal of pharmacology and experimental therapeutics, 369(2), 223-233 (2019-02-26)
We leveraged a clinical pharmacokinetic (PK)/pharmacodynamics (PD)/efficacy relationship established with an oral phosphatidylinositol 3-kinase (PI3K)δ inhibitor (Idelalisib) in a nasal allergen challenge study to determine whether a comparable PK/PD/efficacy relationship with PI3Kδ inhibitors was observed in preclinical respiratory models of
Wanglong Qiu et al.
Clinical cancer research : an official journal of the American Association for Cancer Research, 12(5), 1441-1446 (2006-03-15)
Recent studies have reported high frequencies of somatic mutations in the phosphoinositide-3-kinase catalytic alpha (PIK3CA) gene in several human solid tumors. Although gene amplifications of PIK3CA have been reported in head and neck squamous cell carcinoma (HNSCC), small mutation of
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