Cat. No.: HY-10917

GW2580

13 Cited Publications

Customer Review

Based on 13 publication(s) in Google Scholar

GW2580 is an orally bioavailable and selective inhibitor of c-Fms kinase which completely inhibits human cFMS kinase in vitro at 0.06 μM. GW2580 acts as a competitive inhibitor of ATP binding to the cFMS kinase and inhibits colony-stimulating-factor-1 signaling.

For research use only. We do not sell to patients.

Purity: 99.90%
CAS No.: 870483-87-7
Formula: C₂₀H₂₂N₄O₃
Molecular Weight:366.41

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

GW2580 Chemical Structure

CAS No.: 870483-87-7

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (13)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target

IC50: 60 nM (c-FMS)

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	>30 μM Compound: GW2580	Growth inhibition of serum-stimulated human A549 cells after 3 days by spectrophotometry Growth inhibition of serum-stimulated human A549 cells after 3 days by spectrophotometry	[PMID: 16249345]
BT-474	IC₅₀	21 μM Compound: GW2580	Growth inhibition of serum-stimulated human BT474 cells after 3 days by spectrophotometry Growth inhibition of serum-stimulated human BT474 cells after 3 days by spectrophotometry	[PMID: 16249345]
HFF	IC₅₀	>30 μM Compound: GW2580	Growth inhibition of serum-stimulated HFF after 3 days by spectrophotometry Growth inhibition of serum-stimulated HFF after 3 days by spectrophotometry	[PMID: 16249345]
HN5	IC₅₀	29 μM Compound: GW2580	Growth inhibition of serum-stimulated human HN5 cells after 3 days by spectrophotometry Growth inhibition of serum-stimulated human HN5 cells after 3 days by spectrophotometry	[PMID: 16249345]
HUVEC	IC₅₀	>10 μM Compound: GW2580	Growth inhibition of bFGF-stimulated HUVEC after 3 days by spectrophotometry Growth inhibition of bFGF-stimulated HUVEC after 3 days by spectrophotometry	[PMID: 16249345]
HUVEC	IC₅₀	12 μM Compound: GW2580	Growth inhibition of VEGF-stimulated HUVEC after 3 days by spectrophotometry Growth inhibition of VEGF-stimulated HUVEC after 3 days by spectrophotometry	[PMID: 16249345]
MDA-MB-231	IC₅₀	>30 μM Compound: GW2580	Growth inhibition of serum-stimulated human MDA231 cells after 3 days by spectrophotometry Growth inhibition of serum-stimulated human MDA231 cells after 3 days by spectrophotometry	[PMID: 16249345]
Monocyte	IC₅₀	0.47 μM Compound: GW2580	Growth inhibition of CSF-1-stimulated freshly isolated human monocytes after 3 days by spectrophotometry Growth inhibition of CSF-1-stimulated freshly isolated human monocytes after 3 days by spectrophotometry	[PMID: 16249345]
NCI-N87	IC₅₀	>30 μM Compound: GW2580	Growth inhibition of serum-stimulated human NCI-N87 cells after 3 days by spectrophotometry Growth inhibition of serum-stimulated human NCI-N87 cells after 3 days by spectrophotometry	[PMID: 16249345]
NFS-60	GI₅₀	94 nM Compound: GW-2580	Growth inhibition of mouse NFS60 cells after 72 hrs by CellTiter96 AQueous one solution cell proliferation assay Growth inhibition of mouse NFS60 cells after 72 hrs by CellTiter96 AQueous one solution cell proliferation assay	[PMID: 30522957]
NFS-60	IC₅₀	0.33 μM Compound: GW2580	Growth inhibition of CSF1-stimulated mouse M-NFS-60 cells after 3 days by spectrophotometry Growth inhibition of CSF1-stimulated mouse M-NFS-60 cells after 3 days by spectrophotometry	[PMID: 16249345]
NSO	IC₅₀	13.5 μM Compound: GW2580	Growth inhibition of serum-stimulated mouse NSO cells after 3 days by spectrophotometry Growth inhibition of serum-stimulated mouse NSO cells after 3 days by spectrophotometry	[PMID: 16249345]
Sf21	IC₅₀	3 nM Compound: GW-2580	Antagonist activity at recombinant human N-terminal His6-tagged FMS (538 to end residues) expressed in baculovirus infected Sf21 insect cells using IGF-R1tide as substrate in presence of [gamma-33P]-ATP or [gamma-32P]-ATP Antagonist activity at recombinant human N-terminal His6-tagged FMS (538 to end residues) expressed in baculovirus infected Sf21 insect cells using IGF-R1tide as substrate in presence of [gamma-33P]-ATP or [gamma-32P]-ATP	[PMID: 30522957]

In Vitro

GW2580 completely inhibits the growth of CSF-1-dependent mouse myeloid M-NFS-60 cells at 0.7 μM. GW2580 at 0.8-1 μM completely blocks the ability of CSF-1 to induce the growth of mouse M-NFS60 myeloid cells and human monocytes^[1].
GW2580 causes a 30-40% inhibition of PTH-induced calcium release at 0.1-0.3 μM, with higher concentrations of 1, 3, and 10 μM completely inhibiting the PTH response^[1].
GW2580 inhibits CSF1R phosphorylation in RAW264.7 murine macrophages stimulated with 10 ng/mL with IC₅₀ of approximately 10 nM^[2].
GW2580 also inhibits TRKA activity with IC₅₀ of 0.88 μM^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

GW2580 (Oral administration; 20 and 80 mg/kg) produces a dose-related decrease in the number of tumor cells, with the 80 mg/kg dose completely blocking tumor growth^[1].
GW2580 (Oral administration; 20 and 80 mg/kg) has gave maximal plasma concentrations of 1.4 and 5.6 μM, respectively^[1].
GW2580 (50 mg/kg; twice a day from days 0 to 21, 7 to 21, or 14 to 21) inhibits joint connective tissue and bone destruction in a 21-day adjuvant arthritis model^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Female C3H/HEN mice or female CD-1 nude mice weighing 22-26 g^[1]
Dosage:

20 and 80 mg/kg
Administration:

Oral administration
Result:

Produced a dose-related decrease in the number of tumor cells, with the 80 mg/kg dose completely blocking tumor growth.

Animal Model:

Female C3H/HEN mice or female CD-1 nude mice weighing 22-26 g^[1]
Dosage:

20 and 80 mg/kg (Pharmacokinetic Study)
Administration:

Oral administration
Result:

Had gave maximal plasma concentrations of 1.4 and 5.6 μM, respectively.

Chemical Information

CAS No. 870483-87-7
Appearance Solid
Molecular Weight 366.41
Formula C₂₀H₂₂N₄O₃
Color White to yellow
SMILES

NC1=NC(N)=C(CC2=CC(OC)=C(OCC3=CC=C(OC)C=C3)C=C2)C=N1
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (13)

All WBCell Imaging/StainingIn Vivo ImagingIn Vivo Efficacy Study

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Journal Impact Factor

Nat Biomed Eng

TLR7/8-agonist-loaded nanoparticles promote the polarization of tumour-associated macrophages to enhance cancer immunotherapy. [Abstract]

2018 Aug;2(8):578-588. PMID: 31015631
Bioact Mater

Regulated macrophage immune microenvironment in 3D printed scaffolds for bone tumor postoperative treatment. [Abstract]

2022 May 2;19:474-485. PMID: 35574049

GW2580 purchased from MedChemExpress. Usage Cited in: Bioact Mater. 2022 May 2;19:474-485. [Abstract]

GW2580 (10 μM) exhibited an efficient inhibition of phosphorylation of CSF-1R and phosphorylation of AKT.

GW2580 purchased from MedChemExpress. Usage Cited in: Bioact Mater. 2022 May 2;19:474-485. [Abstract]

Confocal microscope images show mBMSCs morphology on CPC, CPC/hydrogel and CPC/hydrogel/GW2580 (50 mg/kg) scaffolds after 3 days of coculture.

GW2580 purchased from MedChemExpress. Usage Cited in: Bioact Mater. 2022 May 2;19:474-485. [Abstract]

GW2580 (50 mg/kg) loaded scaffolds inhibited tumor growth more efficiently than the untreated and CPC scaffold group by IVIS images.

GW2580 purchased from MedChemExpress. Usage Cited in: Bioact Mater. 2022 May 2;19:474-485. [Abstract]

GW2580 (50 mg/kg)-loaded scaffolds effectively inhibit 4T1 breast tumor growth in a mice model.
J Control Release

Encapsulated cells as an enzyme replacement therapy for metachromatic leukodystrophy. [Abstract]

2025 Oct 11;388(Pt 1):114307. PMID: 41083008
J Control Release

Bioelectronic cell-based device provides a strategy for the treatment of the experimental model of multiple sclerosis. [Abstract]

2022 Dec:352:994-1008. PMID: 36370877
Int Immunopharmacol

CSF-1R inhibition attenuates ischemia-induced renal injury and fibrosis by reducing Ly6C+ M2-like macrophage infiltration. [Abstract]

2020 Nov;88:106854. PMID: 32771945
Cell Signal

CD44-mediated copper accumulation drives Ly6Chi macrophages activation in ulcerative colitis. [Abstract]

2025 Dec 11:112315. PMID: 41389969
Cell Signal

Proguanil inhibits proliferation and migration in glioblastoma development through targeting CSF1R receptor. [Abstract]

2024 Dec 9:111550. PMID: 39662608
BMC Cancer

Artificial intelligence to guide precision anticancer therapy with multitargeted kinase inhibitors. [Abstract]

2022 Nov 24;22(1):1211. PMID: 36434556
J Neurooncol

Medulloblastoma recurrence and metastatic spread are independent of colony-stimulating factor 1 receptor signaling and macrophage survival. [Abstract]

2021 Jun;153(2):225-237. PMID: 33963961
Mol Immunol

The role of neuroplastin65 in macrophage against E. coli infection in mice. [Abstract]

2022 Oct:150:78-89. PMID: 36007354
bioRxiv

Lipid Peroxidation and Type I Interferon Coupling Fuels Pathogenic Macrophage Activation Causing Tuberculosis Susceptibility. [Abstract]

2025 May 1:2024.03.05.583602. PMID: 38496444
Oncotarget

MEK is a promising target in the basal subtype of bladder cancer. [Abstract]

2020 Nov 3;11(44):3921-3932. PMID: 33216841
Cancer Cell Research

22 (2019) 628-637.

Solvent & Solubility

In Vitro:

DMSO : 33.33 mg/mL (90.96 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : < 1 mg/mL (insoluble)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.7292 mL

13.6459 mL

27.2918 mL

5 mM

0.5458 mL

2.7292 mL

5.4584 mL

10 mM

0.2729 mL

1.3646 mL

2.7292 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (5.68 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (5.68 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (5.68 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 0.5% CMC-Na/saline water

Solubility: 5 mg/mL (13.65 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Conway JG, et al. Inhibition of colony-stimulating-factor-1 signaling in vivo with the orally bioavailable cFMS kinase inhibitor GW2580. Proc Natl Acad Sci U S A. 2005 Nov 1;102(44):16078-83. [Content Brief]

[2]. Priceman SJ, et al. Targeting distinct tumor-infiltrating myeloid cells by inhibiting CSF-1 receptor: combating tumor evasion of antiangiogenic therapy. Blood. 2010 Feb 18;115(7):1461-71 [Content Brief]

[3]. Conway JG, et al. Effects of the cFMS kinase inhibitor 5-(3-methoxy-4-((4-methoxybenzyl)oxy)benzyl)pyrimidine-2,4-diamine (GW2580) in normal and arthritic rats. J Pharmacol Exp Ther. 2008 Jul;326(1):41-50. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.7292 mL	13.6459 mL	27.2918 mL	68.2296 mL
	5 mM	0.5458 mL	2.7292 mL	5.4584 mL	13.6459 mL
	10 mM	0.2729 mL	1.3646 mL	2.7292 mL	6.8230 mL
	15 mM	0.1819 mL	0.9097 mL	1.8195 mL	4.5486 mL
	20 mM	0.1365 mL	0.6823 mL	1.3646 mL	3.4115 mL
	25 mM	0.1092 mL	0.5458 mL	1.0917 mL	2.7292 mL
	30 mM	0.0910 mL	0.4549 mL	0.9097 mL	2.2743 mL
	40 mM	0.0682 mL	0.3411 mL	0.6823 mL	1.7057 mL
	50 mM	0.0546 mL	0.2729 mL	0.5458 mL	1.3646 mL
	60 mM	0.0455 mL	0.2274 mL	0.4549 mL	1.1372 mL
	80 mM	0.0341 mL	0.1706 mL	0.3411 mL	0.8529 mL

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GW2580

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Orally Active Compound Library

Targeted Diversity Library

Human Metabolite Library

Membrane Protein-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Macrophage Related Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) GW2580

Biological Activity

Chemical Information

Publications (13)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

GW2580

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Orally Active Compound Library

Targeted Diversity Library

Human Metabolite Library

Membrane Protein-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Macrophage Related Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) GW2580

Biological Activity

Chemical Information

Publications (13)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

GW2580 Related Classifications

Cat. No.: HY-10917