OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Three tyrosine kinase receptors, designated TRKA, TRKB and TRKC, have been identified that selectively bind NGF, BDNF and NT-3, respectively; NT-4/5 also binds to the TRKB receptor. NGF binds to their specific TRK receptor to stimulate intracellular signaling pathways leading to specific protein phosphorylations and differential gene inductions. TRKA (High affinity nerve growth factor, TRK1 transforming tyrosine kinase protein, p140-TrkA, Trk-A) receptor kinases engage the activation of a branched proto-oncoprotein signaling pathway involving Shc, Src, Ras, Raf, mitogen-activated protein kinase, and other downstream effectors. Inhibitors of TRKA may be useful in the treatment of cancer.
Family:
Kinase
Sub Family:
RTK
Class:
Protein Tyrosine
Protein Name:
TRKA
Uniprot Number:
P04629
Protein Aliases:
TRK1-transforming tyrosine kinase protein|Tropomyosin-related kinase A|Tyrosine kinase receptor|Tyrosine kinase receptor A|Trk-A|gp140trk|p140-TrkA|high affinity nerve growth factor receptor
Gene Name:
NTRK1
Gene ID:
4914
Gene Aliases:
TRK|TRKA|MTC
Accession Number:
NM_002529
Organism:
Human
Construct Details:
440-end recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Procedure Summary:
TrkA (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 250 µM KKKSPGEYVNIEFG, 10 mM MgAcetate and [g- 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 KKKSPGEYVNIEFG
Tracer:
33P
ATP Concentration:
[ATP]= 120µM (Km= 129µM )
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:
2
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
Clinical Relevance
Therapeutic Area:
Oncology/Immuno-Oncology
Additional Information
Brand:
LeadHunter
Testing Location:
KP - France - Celle L'Evescault
RELATED SOLUTIONS
TRKA Human RTK Kinase Enzymatic Radiometric [10 uM ATP] KinaseProfiler LeadHunter Assay - FR
Item: 14-571KP10
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