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

GW2580 

Cat. No.: HY-10917 Purity: 99.83%
COA 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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Solution
10 mM * 1 mL in DMSO USD 95 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 95 In-stock
Solid
10 mg USD 86 In-stock
50 mg USD 99 In-stock
100 mg USD 123 In-stock
200 mg USD 185 In-stock
500 mg USD 383 In-stock
1 g USD 581 In-stock
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Customer Review

Based on 10 publication(s) in Google Scholar

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

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  • Customer Review

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

Appearance

Solid

Formula

C20H22N4O3
CAS No.
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 : 33.33 mg/mL (90.96 mM; Need ultrasonic)

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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.83%

COA (246 KB) HNMR (269 KB) LCMS (97 KB)

Handling Instructions (2659 KB)
References
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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.

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The dilution calculator equation

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This equation is commonly abbreviated as: C1V1 = C2V2

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× = ×
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Keywords:

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

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