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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.

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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.

Storage Class Code

11 - Combustible Solids


Certificates of Analysis (COA)

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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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