EGFR Human RTK Kinase Binding Radiometric LeadHunter Assay [10 uM ] - TW

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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:

NM_005228

Organism:

Human

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometry

Measured Response:

Scintillation

Testing Information

Procedure Summary:

Human epidermal growth factor (EGF) receptor endogenously expressed in human epidermoid carcinoma A431 cells are used in modified HEPES buffer pH 7.7. A 0.92 μg‡ aliquot is incubated with 0.08 nM [¹²⁵I]EGF (human) for 60 minutes at 25℃. Non-specific binding is estimated in the presence of 0.1 μM EGF (human). Receptors are filtered and washed, the filters are then counted to determine [¹²⁵I]EGF (human) specifically bound. Compounds are screened at 10 µM.
Note: ‡Membrane protein may change from lot to lot, the concentration used will be adjusted if necessary.

ATP Concentration:

10 uM

Ligand:

[¹²⁵I] EGF (human)

Ligand Kd (nM):

0.17

Ligand Concentration:

0.08 nM

Non Specific:

0.1 µM EGF (human)

Incubation:

60 min at 25°C

Control Inhibitor:

EGF (human)

Criteria For Significance:

≥ 50% of max stimulation or inhibition

Test Concentration / Dose:

Suggested concentration for initial testing is 10 uM

Test Sample Requirements:

Minimum for 1) Screen: 25 μl of 10 mM stock -OR- 1 mg (pre-weighed). 2) Dose Response: 60 μl of 10 mM stock -OR- 1 mg (pre-weighed).

Minimum Order Quantity:

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

Name

EGF (human)

Measurement

0.00053μM - IC50

PubChem ID

Name

TGFo-alpha

Measurement

0.0018μM - IC50

PubChem ID

Name

EGF (murine)

Measurement

0.0023μM - IC50

Clinical Relevance

Therapeutic Area:

Oncology/Immuno-Oncology

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei