EGFR (T790M, L858R) Human RTK Kinase Enzymatic Radiometric [10 uM ATP] KinaseProfiler LeadHunter Assay - FR

Item: 14-721KP10

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OVERVIEW

DOCUMENTS/REFERENCES

Biological Information

Background Information:

Receptors that are tyrosine protein kinases include those receptors for epidermal growth factor (EGF), platelet-derived growth factor (PDGF), insulin, and certain lymphokines. Receptor tyrosine kinases are cell surface transmembrane proteins responsible for intracellular signal transduction. They are expressed in many cell types and, after activation by growth factor binding, trigger a series of intracellular pathways leading to a wide variety of responses; e.g. differentiation, proliferation, migration and invasion, angiogenesis, survival. EGF receptor agonism may facilitate wound healing, enhance viral infections, topical inflammation and asthma as well as tumor cell proliferation and metastasis.

Family:

Kinase

Sub Family:

RTK

Class:

Protein Tyrosine

Protein Name:

EGFR

Uniprot Number:

P00533

Protein Aliases:

erythroblastic leukemia viral (v-erb-b) oncogene homolog (avian)|erb-b2 receptor tyrosine kinase 1

Gene Name:

EGFR

Gene ID:

1956

Gene Aliases:

ERBB1

Accession Number:

X00588

Organism:

Human

Construct Details:

696-end; T790M; L858R recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Enzymatic

Functional Mode:

Antagonist

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Procedure Summary:

EGFR (T790M, L858R) (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 250 µM GGMEDIYFEFMGGKKK, 10 mM MgAcetate and [gamma-33P]-ATP (specific activity and concentration as required). The reaction is initiated by the addition of the Mg/ATP mix. After incubation for 40 minutes at room temperature, the reaction is stopped by the addition of phosphoric acid to a concentration of 0.5%. An aliquot of the reaction is then spotted onto a filter and washed four times for 4 minutes in 0.425% phosphoric acid and once in methanol prior to drying and scintillation counting.

Substrate:

250 µM GGMEDIYFEFMGGKKK

Tracer:

33P

ATP Concentration:

[ATP]= 10µM (Km= 38.73µM )

Incubation:

40 min at Room temperature

Control Inhibitor:

Staurosporine

Test Sample Requirements:

Please provide compounds dissolved in 100% DMSO (PBS or HBSS prohibited).
Stock solution should be ≥50× the final assay concentration (a 10 mM stock is also acceptable).
Required volume:
– <60 kinase assays: 120 µL of 50× stock
– ≥60 assays: 420 µL of 50× stock
If you supply 10 mM stocks or powder (pre-weighed), we will apply the appropriate conversion.
For batches of ~50 compounds supplied as solids, the TAT will be extended.

Minimum Order Quantity:

Turnaround Time

Standard:

6 Business Days

Service Scheduling Note:

Assay is run on a weekly schedule beginning on Friday. Compounds and purchase order must be received on or before 13:00 CET Thursday for the order to be included on the service run that begins on Friday of the same week.

Reference Compound Data

PubChem ID

122130844

Name

Staurosporine

Measurement

0.23nM - IC50

Clinical Relevance

Therapeutic Area:

Oncology/Immuno-Oncology

Adverse / Beneficial Action:

Inhibitors of EGF receptor tyrosine kinase activity may be useful for chemotherapeutic intervention in cases of malignant cellular proliferation.

Additional Information

Brand:

LeadHunter

Testing Location:

KP - France - Celle L'Evescault