GW2580

SKU: orb1305208

Description

GW2580 (SC-203877) is an orally bioavailable, selective inhibitor of the CSF-1R (c-FMS) tyrosine kinase. It is widely used in preclinical research to investigate the role of tumor-associated macrophages in cancer models and to study inflammatory diseases in both in vitro and in vivo experimental settings.

Research Area

Signal Transduction

Key Properties

• CAS Number: 870483-87-7
• MW: 366.41
• Purity: 99.96%
• Formula: C₂₀H₂₂N₄O₃
• SMILES: COc1ccc(COc2ccc(Cc3cnc(N)nc3N)cc2OC)cc1
• Target: c-Fms
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.46 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:8.06 mg/mL (22 mM)

Bioactivity

• Target IC50:
  c-Fms:30 nM
• In Vivo:
  GW2580 effectively inhibits growth in various cell types, demonstrating activity against M-NFS-60 myeloma cells stimulated by CSF-1 (IC50=0.33 μM), NSO myeloma cells stimulated by serum (IC50=13.5 μM), freshly isolated human monocytes stimulated by CSF-1 (IC50=0.47 μM), and human umbilical vein endothelial cells stimulated by vascular endothelial growth factor (IC50=12 μM). It also exhibits inhibitory effects on TRKA (IC50=0.88 μM) and human CFMS kinase (0.06 μM). In RAW264.7 mouse macrophages (IC50=10 nM), GW2580 operates by inhibiting the phosphorylation of CSF1R.
• In Vitro:
  In adjuvant-induced arthritis models, GW2580 (50 mg/kg) effectively inhibits the destruction of joint connective tissue and bone. In mice, the oral administration of GW2580 (40 mg/kg) suppresses the ability of exogenous CSF-1 to enhance lipopolysaccharide-induced TNF-α production. Furthermore, in an intraperitoneal CSF-1 dependent M-NFS-60 tumor cell model, oral GW2580 (80 mg/kg) inhibits tumor cell growth. In transplantable 3LL lung tumor models, GW2580 (160 mg/kg) effectively restricts the growth of bone marrow cells.
• 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)

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SC 203877, SC203877, SC-203877, CSF1R, CSF-1R, CSF-1 receptor, colony stimulating factor 1 receptor, c-Fms, cFms, inhibit, GW 2580, GW2580, GW-2580, Inhibitor

Compound Identifiers

PubChem CID

11617559