CSF1R-IN-28
CSF1R-IN-28 is an orally active CSF-1R inhibitor (IC50 17.2 nM). CSF1R-IN-28 inhibits AKT phosphorylation and reduces the production of inflammatory cytokines (TNF-α, IL-6, and IL-1β). CSF1R-IN-28 dose-dependently alleviates hind paw swelling and arthritis index, and improves histopathological joint damage in adjuvant-induced arthritis rats. CSF1R-IN-28 can be used for research on rheumatoid arthritis.
For research use only. We do not sell to patients.
- CAS No.: 3121274-21-0
- Formula: C24H22F3N3O5
- Molecular Weight:489.44
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
IL-6 |
IL-1β |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | GI50 |
10000 nM
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GI50 > 10,000 nM against parental BaF3 cells assessed as proliferation inhibition after 48 hrs by CellCountingKit-8.
GI50 > 10,000 nM against parental BaF3 cells assessed as proliferation inhibition after 48 hrs by CellCountingKit-8.
|
42721528 |
In Vitro
CSF1R-IN-28 (Compound 11g) (1 h) inhibits CSF-1R kinase in a cell-free ADP-Glo assay (IC50 17.2 nM)[1].
CSF1R-IN-28 (1 μM) showed >90% inhibition of CSF-1R, PDGFRβ, and KIT in a selectivity panel of 78 kinases, with lower inhibition of FLT3, DDR1, and KDR[1].
CSF1R-IN-28 (48 h) selectively inhibits TEL-CSF1R-BaF3 proliferation with a GI50 of 12.89 nM, while having no effect on parental BaF3 cells[1].
CSF1R-IN-28 (0.1-1 μM) dose-dependently inhibits CSF-1-induced p-CSF1R and p-AKT in RAW264.7 macrophages, with significant inhibition at 1 μM[1].
CSF1R-IN-28 (0.1-1 μM; 0.5-1 h) inhibits CSF-1-induced p-CSF1R and p-AKT in RAW264.7 macrophages by immunofluorescence[1].
CSF1R-IN-28 (5-15 μM; 24 h) dose-dependently inhibits LPS-induced release of TNF-α, IL-6, and IL-1β in RAW264.7 macrophages[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:TEL-CSF1R-BaF3 and parental BaF3 cells
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Concentration:Various concentrations
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Incubation Time:48 h
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Result:Inhibited TEL-CSF1R-BaF3 proliferation with GI50 = 12.89 nM and showed no significant inhibitory effect on parental BaF3 cells (GI50 > 10,000 nM).
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Cell Line:RAW264.7 macrophages
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Concentration:0.1, 0.3, and 1 μM
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Incubation Time:0.5-1 h (11g with CSF1); 12 h at 4 °C (primary antibody); 1 h (secondary antibody)
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Result:Reversed CSF-1-induced p-CSF1R and p-AKT to varying degrees at 0.1, 0.3, and 1 μM.
Significantly inhibited p-CSF1R and p-AKT; at 1 μM, p-CSF1R inhibition was comparable to reference compound PLX3397.
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Cell Line:RAW264.7 macrophages
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Concentration:5, 10, 15 μM
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Incubation Time:24 h
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Result:Dose-dependently suppressed TNF-α, IL-6, and IL-1β production in RAW264.7 macrophages, with no obvious cytotoxicity.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (SD) (male)[1]
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Dosage:10 mg/kg; 20 mg/kg; 40 mg/kg
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Administration:p.o. (gavage); daily; from day 12 to day 27
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Result:Decreased hind paw swelling and arthritis index dose-dependently on days 21, 24, and 27.
After 27 days of dosing, 11g at 40 mg/kg showed efficacy comparable to positive control MTX.
In HE-stained ankle joints, 11g reduced inflammatory cell infiltration, improved synovial structure, and limited pannus formation; semi-quantitative grading scores were lower in each 11g dose group (10, 20, 40 mg/kg) than in the AIA model group.
In Safranin O/Fast Green-stained sections, 11g dose-dependently relieved cartilage damage compared with the AIA model group by Mankin scoring.
In AIA rat serum, 11g inhibited TNF-α, IL-6, and IL-1β production in a concentration-dependent manner at 10, 20, and 40 mg/kg.
Chemical Information
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CAS No. 3121274-21-0
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Molecular Weight 489.44
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Formula C24H22F3N3O5
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SMILES
O=C(C1=CN=CO1)N2CCC(OC3=CC(NC(C4=CC=C(OC(F)(F)F)C=C4)=O)=CC=C3C)CC2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CSF1R-IN-28 Related Classifications
HY-189731 Related Classifications
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