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GW2580

Catalog No. T2659   CAS 870483-87-7
Synonyms: GW 2580, SC-203877

GW2580 (SC-203877) is a specific, oral-bioavailable CSF-1R inhibitor for c-FMS.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
GW2580 Chemical Structure
GW2580, CAS 870483-87-7
Pack Size Availability Price/USD Quantity
5 mg In stock $ 43.00
10 mg In stock $ 63.00
50 mg In stock $ 79.00
100 mg In stock $ 98.00
200 mg In stock $ 140.00
500 mg In stock $ 286.00
1 mL * 10 mM (in DMSO) In stock $ 50.00
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Purity: 100%
Purity: 99.48%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description GW2580 (SC-203877) is a specific, oral-bioavailable CSF-1R inhibitor for c-FMS.
Targets&IC50 c-Fms:30 nM
Kinase Assay cFMS tyrosine kinase assay: The enzyme is activated by autophosphorylation by incubating 10 μM enzyme, 100 μM ATP, and 5 mM MgCl2 in 50 mM Tris HCL for 90 min at room temperature. Enzyme reactions are performed in a volume of 45 μL, by using round-bottom polystyrene 96-well plates on a Biomek 2000. Compound in 1 μL DMSO or DMSO alone are added to each well containing 30 μL of a 1.5× substrate reaction mix containing 50 mM Mops (3-[N-Morpholino]propanesulfonic acid), pH 7.5, 15 mM MgCl2, 6 μM peptide substrate, biotin-EAIYAPFAKKK-NH2 7.5 mM DTT, 75 mM NaCl, 10 μM ATP, and 0.5 μCi (1 Ci = 37 GBq) [33P-γ] ATP per assay. The reaction is initiated by the addition of 15 μL of diluted enzyme solution, resulting in a final enzyme concentration 20 nM. EDTA is added to control wells for determination of background. The reaction is allowed to proceed for 40 min and stopped by the addition of an equal volume of 0.5% phosphoric acid, and 75 μL is transferred to a 96-well phosphocellulose filter plate that has been prewet with 100 μL of 0.5% phosphoric acid. The plate is filtered on a Millipore filter-plate vacuum manifold and washed three times with the phosphoric acid solution, followed by the addition of 40 μL of scintillation solution. The plates are sealed and counted in a Packard Topcount NXT scintillation counter.
Cell Research One day before the start of the cell growth assay the cells are spun down and placed in a depleted media at 2× 106 cells per ml for 24 h. Depleted medium for M-NSF60 cells lacks MCSF. The next day, GW2580 at 10 mM in DMSO is diluted to 20 μM and 0.2% DMSO in medium containing 10% serum and serially diluted to yield a 10-point concentration curve. The M-NFS-60 cells are resuspended in medium at 0.5× 106 cells/mL with 10% serum and 20 ng/mL mouse MCSF. Cells (50 μL) are added to each well containing inhibitor (50 μL), and, 3 days later, 10 μL of WST-1 reagent is added to each well. After a 4-h incubation, the absorbance is measured at 440 nm and growth calculated as the difference between wells with full medium and wells with depleted medium.(Only for Reference)
Synonyms GW 2580, SC-203877
Molecular Weight 366.41
Formula C20H22N4O3
CAS No. 870483-87-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 45 mg/mL (122.8 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Conway JG, et al. Proc Natl Acad Sci U S A, 2005, 102(44), 16078-16083. 2. Priceman SJ, et al. Blood, 2010, 115(7), 1461-1471 3. Conway JG, et al. J Pharmacol Exp Ther, 2008, 326(1), 41-50.

Related compound libraries

This product is contained In the following compound libraries:
Tyrosine Kinase Inhibitor Library Highly Selective Inhibitor Library Stem Cell Differentiation Compound Library Bioactive Compounds Library Max Inhibitor Library NO PAINS Compound Library Orally Active Compound Library Kinase Inhibitor Library Bioactive Compound Library Immunology/Inflammation Compound Library

Related Products

Related compounds with same targets
Cerdulatinib hydrochloride c-Fms-IN-2 Anti-Mouse GM-CSF Antibody (MP1-22E9) PF 477736 Onatasertib cFMS Receptor Inhibitor II Ki20227 Pimicotinib

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Keywords

GW2580 870483-87-7 Tyrosine Kinase/Adaptors c-Fms SC203877 inhibit SC 203877 GW-2580 CSF1R GW 2580 CSF-1 receptor Inhibitor SC-203877 CSF-1R colony stimulating factor 1 receptor inhibitor

 

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