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Key Documents

33-047

Sigma-Aldrich

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.

Synonym(s):

3-Step HTRF Assay, PI 3-Kinase Assay

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About This Item

UNSPSC Code:
12161503
eCl@ss:
32161000
NACRES:
NA.84

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

Storage and Stability

12 months at -70°C

Other Notes

Research Category
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.

Pictograms

Exclamation mark

Signal Word

Warning

Hazard Statements

Hazard Classifications

Eye Irrit. 2

Storage Class Code

12 - Non Combustible Liquids

WGK

WGK 2

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


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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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
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

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