Biological Information
Background Information:
CSF1R (colony stimulating factor I receptor), formerly known as FMS (McDonough feline sarcoma viral oncogene), is a receptor tyrosine kinase for CSF-1 and expressed primarily in monocytes, macrophages, and human tumor tissue. CSF-1 binding to FMS induces dimerization of the tyrosine kinase domain of the receptor, and stimulates the survival, proliferation, and differentiation of haematopoietic cells of the monocyte-macrophage series.
Family:
Kinase
Sub Family:
RTK
Class:
Protein Tyrosine
Protein Name:
Fms (CSFR)
Uniprot Number:
P07333
Protein Aliases:
CSF-1-R|CSF-1R|M-CSF-R|Proto-oncogene c-Fms|CD antigen CD115
Gene Name:
CSF1R
Gene ID:
1436
Gene Aliases:
C-FMS|CSFR|CD115
Accession Number:
U63963
Organism:
Human
Construct Details:
538-end recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Procedure Summary:
Fms (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]= 10µM (Km= 985µM )
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 CSF1R may be useful in the treatment of breast, ovarian cancer and a variety of epithelial tumors.
Additional Information
Brand:
LeadHunter
Testing Location:
KP - France - Celle L'Evescault
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