Biological Information

Background Information:

Fibroblast growth factor (FGF) superfamily consists of 23 members, all of which contain a conserved 120 amino acid (aa) core region that contains six identical, interspersed amino acids. Based on the pI factor, two main groups of FGF are named: acidic FGF (aFGF) and basic FGF (bFGF). The superfamily members act extracellularly through four tyrosine kinase FGF receptors (FGR1 through FGR4), with multiple specificities noted for almost all FGFs. Biological binding of aFGF to its receptors will result in phosphorylation of the receptor and non-receptor proteins and generate its function. FGR2 (FGFR-2, Fibroblast growth factor receptor 2, Keratinocyte growth factor receptor 2, EC 2.7.1.112) is expressed mainly in bone, central nervous system, smooth muscle and tumors. Inhibition of FGR2 may inhibit cranial development and arterial repair as well as facilitate formation and proliferation of some tumors (e.g., prostate, thyroid).

Family:

Kinase

Sub Family:

RTK

Class:

Protein Tyrosine

Protein Name:

FGFR2

Uniprot Number:

P21802

Protein Aliases:

Crouzon syndrome|Pfeiffer syndrome

Gene Name:

FGFR2

Gene ID:

2263

Gene Aliases:

CEK3|TK14|TK25|ECT1|K-SAM|CD332|BEK|KGFR|KSAM

Accession Number:

NM_022976

Organism:

Human

Construct Details:

Fragment (456-770), Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Enzymatic

Functional Mode:

Antagonist

Detection Method:

Radiometry

Measured Response:

Scintillation

Testing Information

Procedure Summary:

Human recombinant protein kinase FGFR2 expressed in insect Sf21 cells is used. Test compound and/or vehicle is preincubated with 0.1 U/ml enzyme‡ in modified HEPES buffer pH 7.4 for 15 minutes at 37°C. The reaction is initiated by addition of 200 μg/ml poly(Glu:Tyr), 10 μM ATP and 0.25 μCi [γ32P]ATP for another 30 minute incubation period and terminated by further addition of 3% H3PO4. An aliquot is removed and counted to determine the amount of [32P]Poly(Glu:Tyr) formed. Compounds are screened at 10 μM.

Substrate:

200 µg/ml Poly(Glu:Tyr)

ATP Concentration:

10 uM

Incubation:

30 min at 37°C

Control Inhibitor:

Staurosporine

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:

2

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

5328760

Name

Tyrphostin AG 538

Measurement

0.44μM - IC50

PubChem ID

122130844

Name

Staurosporine

Measurement

0.0051μM - IC50

Clinical Relevance

Therapeutic Area:

Oncology/Immuno-Oncology

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

RELATED SOLUTIONS

Item: PP90