GW2580

Catalog No.S8042 Synonyms: SC-203877

For research use only.

GW2580 (SC-203877) is a selective CSF-1R inhibitor for c-FMS with IC50 of 30 nM, 150- to 500-fold selective compared to b-Raf, CDK4, c-KIT, c-SRC, EGFR, ERBB2/4, ERK2, FLT-3, GSK3, ITK, JAK2 etc.

GW2580 Chemical Structure

CAS No. 870483-87-7

Selleck's GW2580 has been cited by 13 publications

Purity & Quality Control

Choose Selective CSF-1R Inhibitors

Biological Activity

Description GW2580 (SC-203877) is a selective CSF-1R inhibitor for c-FMS with IC50 of 30 nM, 150- to 500-fold selective compared to b-Raf, CDK4, c-KIT, c-SRC, EGFR, ERBB2/4, ERK2, FLT-3, GSK3, ITK, JAK2 etc.
Targets
c-Fms [1]
30 nM
In vitro

GW2580 completely inhibits human cFMS kinase in vitro at 0.06 μM. GW2580 inhibits the growth of CSF-1 stimulated M-NFS-60 myeloid tumor cells, serum stimulated NSO myeloid tumor cells, CSF-1 stimulated freshly isolated human monocytes, and VEGF stimulated human umbilical vein vascular endothelial cells with IC50 of 0.33, 13.5, 0.47 and 12 μM, respectively. 1 μM GW2580 completely inhibits CSF-1-induced growth of mouse M-NFS-60 myeloid cells and human monocytes and completely inhibits bone degradation in cultures of human osteoclasts, rat calvaria, and rat fetal long bone. [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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HUVEC M1L3dmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2jqNWdzd3e2aDDpcohq[mm2aX;uJI9nKF[HR1[td5RqdXWuYYTl[EBJXV[HQzDh[pRmeiB|IHThfZMh[nlic4DlZ5Rzd3Cqb4TvcYV1enl? NXK3dnV3OTZ{NEmzOFU>
mouse NSO cells MmL2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1;N[2dzd3e2aDDpcohq[mm2aX;uJI9nKHOncoXtMZN1cW23bHH0[YQhdW:3c3WgUnNQKGOnbHzzJIFnfGW{IEOg[IF6eyCkeTDzdIVkfHKxcHjveI9u\XS{eTygTWM2OD1zMz61JO69VQ>? M2[1blE3OjR7M{S1
human BT474 cells NE\ye5lIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYnHdo94fGhiaX7obYJqfGmxbjDv[kB{\XK3bT3zeIlufWyjdHXkJIh2dWGwIFLUOFc1KGOnbHzzJIFnfGW{IEOg[IF6eyCkeTDzdIVkfHKxcHjveI9u\XS{eTygTWM2OD1{MTFOwG0> NIjjOHQyPjJ2OUO0OS=>
human HN5 cells M1vTZmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWPHdo94fGhiaX7obYJqfGmxbjDv[kB{\XK3bT3zeIlufWyjdHXkJIh2dWGwIFjOOUBk\WyuczDh[pRmeiB|IHThfZMh[nlic4DlZ5Rzd3Cqb4TvcYV1enluIFnDOVA:OjlizszN MVWxOlI1QTN2NR?=
human PBMC Ml;aSpVv[3Srb36gZZN{[Xl? M{jVdWlvcGmkaYTpc44hd2ZiTGDTMYlv\HWlZXSgTWw3KHC{b3T1Z5Rqd25iaX6gbJVu[W5iUFLNR{BjgSCHTFnTRUwhTUN3ME2xMlg6KM7:TR?= NHXtZoUzOzB7NUC0NS=>
In vivo GW2580 (dosed orally at 40 mg/kg 0.5 h before the CSF-1-priming dose) blocks the ability of exogenous CSF-1 to increase LPS-induced TNF-α production in mice by 63%. When given to mice before CSF-1 priming, GW2580 completely blocks the ability of CSF-1 to prime the mouse for increased IL-6 production. GW2580 (80 mg/kg p.o.) completely inhibits the growth of CSF-1-dependent M-NFS-60 tumor cells in the peritoneal cavity. GW2580 (80 mg/kg) dosed orally twice a day the week before thioglycolate injection and for the 4-day period after thioglycolate injection, diminishes the accumulation of macrophages in the peritoneal cavity after thioglycolate injection (by 45%). [1] In a 21-day adjuvant arthritis model, GW2580 (50 mg/kg) dosed twice a day from days 0 to 21, 7 to 21, or 14 to 21 inhibits joint connective tissue and bone destruction. [3] Gw2580 (160 mg/kg) induces a more than 2-fold reduction of total CD45+ CD11b+ myeloid cells, CD11b+ F4/80+ TAMs, and CD11b+ Gr-1+ MDSCs in implanted 3LL lung tumor, through inhibiting tumor recruitment of myeloid cells from peripheral blood. GW2580 (80 mg/kg) treatment is able to suppress Vegf-a (by 35%) and Mmp9 (by 70%) expression, as well as tumor vascular density (CD31 staining). Combination therapy with GW2580 and an anti-VEGFR-2 antibody results in synergistic tumor growth reduction. DC101 alone reduces tumor growth by 35%, the combination of DC101 and GW2580 results in an apparent synergistic tumor growth reduction of approximately 70%. [2]

Protocol (from reference)

Kinase Assay:[1]
  • cFMS tyrosine kinase assay:

    The enzyme is activated by autophosphorylation by incubating 10 μM enzyme, 100 μM ATP, and 5 mM MgCl2 in 50 mM Tris HCL for 90 min at room temperature. Enzyme reactions are performed in a volume of 45 μL, by using round-bottom polystyrene 96-well plates on a Biomek 2000. Compound in 1 μL DMSO or DMSO alone are added to each well containing 30 μL of a 1.5× substrate reaction mix containing 50 mM Mops (3-[N-Morpholino]propanesulfonic acid), pH 7.5, 15 mM MgCl2, 6 μM peptide substrate, biotin-EAIYAPFAKKK-NH2 7.5 mM DTT, 75 mM NaCl, 10 μM ATP, and 0.5 μCi (1 Ci = 37 GBq) [33P-γ] ATP per assay. The reaction is initiated by the addition of 15 μL of diluted enzyme solution, resulting in a final enzyme concentration 20 nM. EDTA is added to control wells for determination of background. The reaction is allowed to proceed for 40 min and stopped by the addition of an equal volume of 0.5% phosphoric acid, and 75 μL is transferred to a 96-well phosphocellulose filter plate that has been prewet with 100 μL of 0.5% phosphoric acid. The plate is filtered on a Millipore filter-plate vacuum manifold and washed three times with the phosphoric acid solution, followed by the addition of 40 μL of scintillation solution. The plates are sealed and counted in a Packard Topcount NXT scintillation counter.

Cell Research:[1]
  • Cell lines: MCSF-dependent mouse myeloid M-NFS-60 cell line
  • Concentrations: ~20 μM
  • Incubation Time: 3 days
  • Method: One day before the start of the cell growth assay the cells are spun down and placed in a depleted media at 2× 106 cells per ml for 24 h. Depleted medium for M-NSF60 cells lacks MCSF. The next day, GW2580 at 10 mM in DMSO is diluted to 20 μM and 0.2% DMSO in medium containing 10% serum and serially diluted to yield a 10-point concentration curve. The M-NFS-60 cells are resuspended in medium at 0.5× 106 cells/mL with 10% serum and 20 ng/mL mouse MCSF. Cells (50 μL) are added to each well containing inhibitor (50 μL), and, 3 days later, 10 μL of WST-1 reagent is added to each well. After a 4-h incubation, the absorbance is measured at 440 nm and growth calculated as the difference between wells with full medium and wells with depleted medium.
Animal Research:[1]
  • Animal Models: Mouse myeloid carcinoma xenografts M-NFS-60
  • Dosages: 80 mg/kg
  • Administration: Orally twice a day

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
5% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.

5mg/mL

Chemical Information

Molecular Weight 366.41
Formula

C20H22N4O3

CAS No. 870483-87-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles COC1=CC=C(C=C1)COC2=C(C=C(C=C2)CC3=CN=C(N=C3N)N)OC

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

Question 1:
How to reconstitute the inhibitor for i.p. injection in mice?

Answer:
It can be dissolved in 5% DMSO/30% PEG 300/5% Tween 80/ddH2O at 5 mg/ml clearly. When prepare this kind of vehicle, please dissolve the drug in DMSO clearly first, then add PEG and Tween. After they mixed homogeneously, then dilute with water.

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