OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Insulin-like growth factor (IGF) binding to the IGF receptors initiates an intracellular signaling cascade that leads to changes in gene expression and cell biology. Although multiple receptors for the IGFs have been identified, the IGFs primarily exert their biologic effects through ligation of the IGF1R (type I IGF receptor tyrosine kinase, JTK13). IGF1R exerts mitogenic, cell survival, and insulin-like activities, is involved in postnatal growth physiology, and is connected to proliferative disorders such as breast cancer.
Family:
Kinase
Sub Family:
RTK
Class:
Protein Tyrosine
Protein Name:
IGF1R
Uniprot Number:
P08069
Protein Aliases:
Insulin-like growth factor I receptor|IGF-I receptor|CD antigen CD221 [Cleaved into: Insulin-like growth factor 1 receptor alpha chain; Insulin-like growth factor 1 receptor beta chain]
Gene Name:
IGF1R
Gene ID:
3480
Gene Aliases:
JTK13|CD221|IGFIR|MGC18216|IGFR
Accession Number:
X04434
Organism:
Human
Construct Details:
959-end recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Procedure Summary:
IGF-1R (h) is incubated with 50 mM Tris pH 7.5, 0.1 mM EGTA, 0.1 mM Na3VO4, 0.1% 6-mercaptoethanol, 250 µM KKKSPGEYVNIEFG, 10 mM MnCl2, 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 KKKSPGEYVNIEFG
Tracer:
33P
ATP Concentration:
[ATP]= 200µM (Km= 497µM )
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
Adverse / Beneficial Action:
Inhibition of IGF1R may inhibit growth, motility and protection from apoptosis in many tumors.
Additional Information
Brand:
LeadHunter
Testing Location:
KP - France - Celle L'Evescault
RELATED SOLUTIONS
IGF1R Human RTK Kinase Enzymatic Radiometric [10 uM ATP] KinaseProfiler LeadHunter Assay - FR
Item: 14-465KP10
IGF1R (activated) Human RTK Kinase Enzymatic Radiometric [Km ATP] KinaseProfiler LeadHunter Assay - FR
Item: 14-802KP
IGF1R (activated) Human RTK Kinase Enzymatic Radiometric [10 uM ATP] KinaseProfiler LeadHunter Assay - FR
Item: 14-802KP10
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