1. Protein Tyrosine Kinase/RTK
  2. c-Fms
  3. GW2580

GW2580 

Cat. No.: HY-10917 Purity: 99.44%
Handling Instructions

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

GW2580 Chemical Structure

CAS No. : 870483-87-7

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 86 In-stock
Estimated Time of Arrival: December 31
10 mg USD 78 In-stock
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50 mg USD 90 In-stock
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100 mg USD 112 In-stock
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200 mg USD 168 In-stock
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500 mg USD 348 In-stock
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1 g USD 528 In-stock
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Customer Review

Based on 5 publication(s) in Google Scholar

Top Publications Citing Use of Products
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Description

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[1].

IC50 & Target

IC50: 60 nM (c-FMS)

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].

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].

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

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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 17.5 mg/mL (47.76 mM; Need ultrasonic and warming)

Ethanol : < 1 mg/mL (insoluble)

H2O : < 0.1 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.5 mg/mL (6.82 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.44%

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Keywords:

GW2580GW 2580GW-2580c-FmsCSF-1 receptorcolony stimulating factor 1 receptorCSF-1RCSF1RInhibitorinhibitorinhibit

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GW2580
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HY-10917
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