GW2580

Name: GW2580
Brand: MedChemExpress
SKU: HY-10917
Rating: 5.0 (12 reviews)

Cat. No.: HY-10917 Purity: 99.90%: FAQs
Data Sheet
SDS

COA
Handling Instructions Technical Support

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.

GW2580 Chemical Structure

CAS No. : 870483-87-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
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Customer Review

Based on 12 publication(s) in Google Scholar

Other Forms of GW2580:

GW2580-d₆ Get quote

12 Publications Citing Use of MCE GW2580

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Biological Activity
Purity & Documentation
References
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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	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]
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]
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.

Molecular Weight

366.41

Formula

C₂₀H₂₂N₄O₃

CAS No.

870483-87-7

Appearance

Solid

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

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.
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.

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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.90%

Select Batch:

Data Sheet (277 KB) SDS (393 KB)

COA (246 KB) HNMR (269 KB) LCMS (94 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]

Complete Stock Solution Preparation Table

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

GW2580 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GW2580870483-87-7GW 2580GW-2580c-FmsCSF-1 receptorcolony stimulating factor 1 receptorCSF-1RCSF1RInhibitorinhibitorinhibit

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GW2580

Customer Review

Other Forms of GW2580:

GW2580 Related Antibodies

12 Publications Citing Use of MCE GW2580

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•Related Screening Libraries:

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•Related Proteins:

Biological Activity

Purity & Documentation

References

Customer Review

GW2580 Related Antibodies

Molarity Calculator

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Complete Stock Solution Preparation Table

GW2580 Related Classifications

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