GW2580
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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.90%
- CAS No.: 870483-87-7
- Formule: C20H22N4O3
- Masse moléculaire:366.41
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) GW2580
More- Nat Biomed Eng. 2018 Aug;2(8):578-588. [Abstract]
- Bioact Mater. 2022 May 2;19:474-485. [Abstract]
- J Control Release. 2025 Oct 11;388(Pt 1):114307. [Abstract]
- J Control Release. 2022 Dec:352:994-1008. [Abstract]
- Int Immunopharmacol. 2020 Nov:88:106854. [Abstract]
- Cell Signal. 2025 Dec 11:112315. [Abstract]
- Cell Signal. 2025 Mar:127:111550. [Abstract]
- BMC Cancer. 2022 Nov 24;22(1):1211. [Abstract]
- Mol Immunol. 2022 Oct:150:78-89. [Abstract]
- J Neurooncol. 2021 Jun;153(2):225-237. [Abstract]
- bioRxiv. 2025 May 1:2024.03.05.583602. [Abstract]
- Oncotarget. 2020 Nov 3;11(44):3921-3932. [Abstract]
- Cancer Cell Research. 22 (2019) 628-637.
Customer Validation & Images
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WB
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Cell Imaging/Staining
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In Vivo Imaging
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In Vivo Efficacy Study
Activité biologique
IC50: 60 nM (c-FMS)
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Cell Line
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Type | Value | Description | References |
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| A549 | IC50 |
>30 μM
Compound: GW2580
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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
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[PMID: 16249345] |
| BT-474 | IC50 |
21 μM
Compound: GW2580
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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
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[PMID: 16249345] |
| HFF | IC50 |
>30 μM
Compound: GW2580
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Growth inhibition of serum-stimulated HFF after 3 days by spectrophotometry
Growth inhibition of serum-stimulated HFF after 3 days by spectrophotometry
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[PMID: 16249345] |
| HN5 | IC50 |
29 μM
Compound: GW2580
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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
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[PMID: 16249345] |
| HUVEC | IC50 |
>10 μM
Compound: GW2580
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Growth inhibition of bFGF-stimulated HUVEC after 3 days by spectrophotometry
Growth inhibition of bFGF-stimulated HUVEC after 3 days by spectrophotometry
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[PMID: 16249345] |
| HUVEC | IC50 |
12 μM
Compound: GW2580
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Growth inhibition of VEGF-stimulated HUVEC after 3 days by spectrophotometry
Growth inhibition of VEGF-stimulated HUVEC after 3 days by spectrophotometry
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[PMID: 16249345] |
| MDA-MB-231 | IC50 |
>30 μM
Compound: GW2580
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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
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[PMID: 16249345] |
| Monocyte | IC50 |
0.47 μM
Compound: GW2580
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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
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[PMID: 16249345] |
| NCI-N87 | IC50 |
>30 μM
Compound: GW2580
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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
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[PMID: 16249345] |
| NFS-60 | GI50 |
94 nM
Compound: GW-2580
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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
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[PMID: 30522957] |
| NFS-60 | IC50 |
0.33 μM
Compound: GW2580
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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
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[PMID: 16249345] |
| NSO | IC50 |
13.5 μM
Compound: GW2580
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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
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[PMID: 16249345] |
| Sf21 | IC50 |
3 nM
Compound: GW-2580
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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
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[PMID: 30522957] |
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.
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.
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Animal Model:Female C3H/HEN mice or female CD-1 nude mice weighing 22-26 g[1]
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Dosage:20 and 80 mg/kg
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Administration:Oral administration
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Result:Produced a dose-related decrease in the number of tumor cells, with the 80 mg/kg dose completely blocking tumor growth.
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Animal Model:Female C3H/HEN mice or female CD-1 nude mice weighing 22-26 g[1]
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Dosage:20 and 80 mg/kg (Pharmacokinetic Study)
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Administration:Oral administration
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Result:Had gave maximal plasma concentrations of 1.4 and 5.6 μM, respectively.
Chemical Information
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CAS No. 870483-87-7
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Appearance Solid
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Masse moléculaire 366.41
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Formule C20H22N4O3
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Color White to yellow
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SMILES
NC1=NC(N)=C(CC2=CC(OC)=C(OCC3=CC=C(OC)C=C3)C=C2)C=N1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (13)
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Journal Impact Factor
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Most Recent
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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.
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J Control Release
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]2025 Mar:127:111550. PMID: 39662608 -
BMC Cancer
Artificial intelligence to guide precision anticancer therapy with multitargeted kinase inhibitors. [Abstract]2022 Nov 24;22(1):1211. PMID: 36434556 -
Mol Immunol
2022 Oct:150:78-89. PMID: 36007354 -
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 -
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
2020 Nov 3;11(44):3921-3932. PMID: 33216841 -
Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Add each solvent one by one: 0.5% CMC-Na/saline water
Solubility: 5 mg/mL (13.65 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (277 KB)
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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)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[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]
Complete Stock Solution Preparation Table
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| 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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