Structure of GW2580
CAS No.: 870483-87-7
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
GW2580 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.
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CAS No. : | 870483-87-7 |
Formula : | C20H22N4O3 |
M.W : | 366.41 |
SMILES Code : | NC1=NC=C(CC2=CC=C(OCC3=CC=C(OC)C=C3)C(OC)=C2)C(N)=N1 |
MDL No. : | MFCD12024701 |
InChI Key : | MYQAUKPBNJWPIE-UHFFFAOYSA-N |
Pubchem ID : | 11617559 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H302-H315-H319-H335 |
Precautionary Statements: | P261-P305+P351+P338 |
In Vitro:
Cell Line
|
Concentration | Treated Time | Description | References |
Human osteoclasts | 1 μM | 3 days | Inhibited bone degradation and actin-ring formation | PMC1276040 |
Freshly isolated human monocytes | 0.47 μM | 5 days | Completely inhibited CSF-1-induced growth | PMC1276040 |
Mouse myeloid NS0 cells | 13.5 μM | No significant effect on CSF-1-independent cell growth | PMC1276040 | |
Mouse myeloid M-NFS-60 cells | 0.33 μM | Completely inhibited CSF-1-induced cell growth | PMC1276040 | |
Human islet cells | 10 mg/ml | Assess toxicity of GW2580 on human islet cells | PMC7184801 | |
Mouse satellite glial cells (SGCs) | 20 mg/mL | 1, 3, 7 days | To evaluate the effect of PLGA and PLGAM microparticles on the proliferation of SGCs, results showed no significant effect on cell proliferation. | PMC10066835 |
Human adipose mesenchymal stem cells (ADMSCs) | 20 mg/mL | 1, 3, 7 days | To evaluate the effect of PLGA and PLGAM microparticles on the proliferation of ADMSCs, results showed no significant effect on cell proliferation. | PMC10066835 |
Mouse bone marrow mesenchymal stem cells (mBMSCs) | 10 μM | 24 and 72 hours | To study the effect of GW2580 on mBMSCs proliferation, adhesion, and osteogenic differentiation. Results showed that GW2580 did not affect mBMSCs function at the later stage of release and promoted osteogenesis. | PMC9079115 |
Mouse bone marrow-derived monocytes (BMMs) | 10 μM | 24 and 72 hours | To study the inhibitory effect of GW2580 on BMMs proliferation and osteoclast differentiation. Results showed that GW2580 significantly inhibited BMMs proliferation and osteoclast differentiation. | PMC9079115 |
Human peripheral blood mononuclear cells | 470 nM or 4.7 μM | 24 hours | To investigate the effect of GW2580 on M-CSF or IL-34-induced CD163 and CD16 expression, results showed GW2580 could inhibit the expression of these markers | PMC4381451 |
Rhesus macaque peripheral blood mononuclear cells | 470 nM or 4.7 μM | 24 hours | To investigate the effect of GW2580 on M-CSF or IL-34-induced CD163 and CD16 expression, results showed GW2580 could inhibit the expression of these markers | PMC4381451 |
RAW264.7 cells | 10 μM | 4 hours | To study the inhibitory effect of GW2580 on CSF-1R and NF-κB signaling pathways. Results showed that released GW2580 effectively inhibited phosphorylation of CSF-1R and significantly attenuated phosphorylation of AKT and NF-κB signaling pathways. | PMC9079115 |
RAW 264.7 cells | 10–1000 nM | 48 hours | GW2580 reduced MCSF-stimulated production of TNF to basal levels. | PMC3225802 |
Primary microglia | 5 µM | 48 hours | To assess GW2580's effect on LPS-activated microglial viability. Results showed combined GW2580 and LPS treatment significantly reduced cell viability in a ROS-dependent manner. | PMC8664563 |
Primary microglia | 5 µM | 48 hours | To evaluate the effect of GW2580 on microglial proliferation. Results showed GW2580 dose-dependently inhibited CSF1-induced cell proliferation without affecting viability. | PMC8664563 |
Freshly isolated human monocytes | 0.47 μM (IC50) | 5 days | Completely inhibited CSF-1-induced growth | PMC1276040 |
Mouse myeloid NS0 cells | 13.5 μM (IC50) | No significant effect on CSF-1-independent cell growth | PMC1276040 | |
Mouse myeloid M-NFS-60 cells | 0.33 μM (IC50) | Completely inhibited CSF-1-induced cell growth | PMC1276040 |
In Vivo:
Species
|
Animal Model
|
Administration | Dosage | Frequency | Description | References |
Mice | Chronic cerebral hypoperfusion model | Oral | 0.1% (1000 ppm) | 6 weeks | GW2580 treatment prevented the expansion of microglial numbers in chronic hypoperfused white matter, attenuated hypoperfusion-induced white matter pathology, and rescued spatial learning impairments and to a lesser extent cognitive flexibility. | PMC10952452 |
Mice | Chronic DRA-induced asthma model | Intranasal administration | 1 ng/mouse | Twice a week for 6 weeks | Intranasal delivery of CDPL-GW nanoprobe significantly ameliorated asthma pathologies including allergen-specific serum IgE production, allergic lung and airway inflammation and airway hyper-responsiveness (AHR) with minimal pulmonary adverse reaction. | PMC7002247 |
C57BL/6 mice | Diabetic model | Intraperitoneal and subcutaneous implantation | 10 mg/ml | Up to 15 months | Evaluate long-term anti-fibrotic effects and glycemic control of GW2580 in diabetic models | PMC7184801 |
Mice | Nephritis model | Oral gavage | 100 mg/kg | Once daily for 10 days | GW2580 treatment ameliorated proteinuria and renal dysfunction in the nephritis model, reduced glomerular macrophage infiltration, and decreased the expression of inflammatory cytokines. | PMC4323927 |
C57BL/6 mice | Experimental autoimmune encephalomyelitis (EAE) model | Oral | 100 mg/kg | Every 12 hours until the end of the experiment | GW2580 ameliorated the severity of EAE, reduced the proportion of macrophages in the CNS, and decreased circulating TNF levels. | PMC3225802 |
CX3CR1+/eGFP transgenic mice | Spinal cord injury model | Oral | 150 mg/kg/day | 1 week | GW2580 treatment reduced microglia proliferation, improved motor function recovery, and promoted tissue protection. | PMC8419033 |
Mice | Breast cancer model | Oral gavage | 160 mg/kg | Daily, starting one day after tumor cell inoculation | GW2580 inhibited macrophage infiltration and function, reversing stress-enhanced metastasis | PMC2940980 |
C57BL/6 mice | ID8 epithelial ovarian cancer model | Oral | 160 mg/kg | Once daily for 2 weeks | GW2580 treatment reduced infiltration of M2 macrophages, dramatically decreased ascites volume, and normalized the peritoneal vasculature. | PMC4675660 |
Athymic nude mice | Orthotopic U251 glioma model | Oral | 160 mg/kg/day | Daily for two weeks | GW2580 significantly reduced tumor growth, decreased infiltration of GFP+ BMDCs in the tumor microenvironment, and reduced myeloid (Gr1+ CD11b+ and F4/80+) and angiogenic (CD202b+ and VEGFR2+) cell signatures. | PMC4686232 |
Mice | C3H/HEN mice and CD-1 nude mice | Oral | 20 and 80 mg/kg | Twice daily for 4 days | Inhibited CSF-1-dependent tumor cell growth and macrophage accumulation | PMC1276040 |
Dark agouti (DA) female rats | Experimental allergic encephalomyelitis (EAE) | Oral gavage | 40 mg/kg | Once daily for 11 days | GW2580 treatment delayed the onset of the disease, significantly reduced the clinical severity, and prevented the relapse phase | PMC5111339 |
Dark Agouti rats | Experimental Autoimmune Encephalomyelitis (EAE) | Oral gavage | 40 mg/kg | Daily from day -1 to day 11 after immunization | GW2580 treatment decreased EAE clinical severity and prevents the relapse phase, reduced microglial proliferation and T-cell infiltration, and preserved BBB integrity. | PMC11941641 |
BALB/c mice | 4T1 breast tumor model | Subcutaneous implantation | 50 mg/kg | Single implantation, lasting for 10 days | To study the anti-tumor effect and immunoregulatory role of GW2580-loaded scaffolds in vivo. Results showed that GW2580-loaded scaffolds significantly reduced the proportion of M2-type macrophages in the tumor and inhibited tumor growth. | PMC9079115 |
Microcebus murinus | Spinal cord injury model | Oral | 7.2 mg/day | 2 weeks | GW2580 treatment reduced microglia proliferation, improved motor function recovery, and promoted tissue protection. | PMC8419033 |
Mice | Influenza A virus infection model | Oral gavage | 80 mg/kg/day | Once daily for 15 days | Evaluate reversal effect of CSF1R antagonist on infection-induced oligodendrocyte transcriptional changes | PMC10439573 |
C57BL/6J mice | Healthy mice | Oral gavage | 80 mg/kg/day | Once daily for 8 days | To evaluate GW2580's effects on microglial morphology and function in healthy mice. Results showed GW2580 altered microglial morphology without affecting cell numbers or circulating immune cell percentages. RNA-seq analysis revealed downregulation of ROS-related genes. | PMC8664563 |
Bio Calculators | ||||
Preparing Stock Solutions | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.73mL 0.55mL 0.27mL |
13.65mL 2.73mL 1.36mL |
27.29mL 5.46mL 2.73mL |
Tags: GW2580 | GW 2580 | GW-2580 | c-Fms | CSF-1 receptor | colony stimulating factor 1 receptor | CSF-1R | CSF1R | c-Fms kinase inhibitor | ATP competitive inhibitor | colony-stimulating-factor-1 signaling | kinase inhibitor | receptor tyrosine kinase | PI3K/Akt | MAPK | STAT pathway | 870483-87-7
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