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GW-2580

SKU: orb1305208
FeaturedFeatured Product

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

Immunology & Inflammation

Images & Validation

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GW-2580

Key Properties

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CAS Number870483-87-7
MW366.32
Purity>98%
FormulaC20H22N4O3
SMILESCOc1ccc(COc2ccc(Cc3cnc(N)nc3N)cc2OC)cc1
TargetKinase
SolubilitySoluble in DMSO (up to 40 mg/ml).

Bioactivity

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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.
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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.
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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)
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Storage & Handling

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StorageRT
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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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

Similar Products

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  • GW2580

    GW2580 [orb1223794]

    >98% (HPLC)

    870483-87-7

    366.4137

    C20H22N4O3

    1 g, 5 mg, 500 mg, 10 mg, 100 mg, 200 mg, 50 mg
Quality Guarantee

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at [email protected].

Compound Identifiers

PubChem CID
11617559 ↗

Key Properties

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No computed properties available.

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GW-2580 (orb1305208)

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Step 1: Enter information below

(Recommended: An additional animal making an allowance for loss during the experiment)

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% DMSO +
%+
% Tween 80 +
%

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5 mg
¥ 2,730.00
25 mg
¥ 5,980.00
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