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| Targets |
c-Fms-IN-3 targets the c-Fms (CSF1R) kinase, inhibiting its activity. This inhibition reduces macrophage populations. By blocking CSF1R signaling, it modulates the immune microenvironment and bone resorption. It is used as a preclinical research tool to study tumor-associated macrophages, osteoclastogenesis, and inflammatory diseases.
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| ln Vitro |
In vitro, c-Fms-IN-3 demonstrates potent inhibition of CSF1R kinase activity. This leads to a reduction in macrophage populations in cell-based assays. Its activity is confirmed in kinase assays where it inhibits the phosphorylation of CSF1R and its downstream substrates. Its potential as an anti-inflammatory and antirheumatic agent is supported by these findings.
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| ln Vivo |
In vivo, c-Fms-IN-3 has shown efficacy in preclinical models. In a collagen-induced arthritis mouse model, it reduces bone erosion, pannus invasion, cartilage damage, and inflammation. This demonstrates its potential as a therapeutic agent for rheumatoid arthritis and other inflammatory diseases.
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| Enzyme Assay |
The in vitro kinase assay for c-Fms-IN-3 involves measuring its ability to inhibit the phosphorylation activity of CSF1R. The enzyme is incubated with a peptide substrate and ATP in the presence of varying concentrations of the compound. The amount of phosphorylated substrate is measured using a luminescent or fluorescent detection system, and the IC50 is calculated from the dose-response curve.
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| Cell Assay |
In vitro cell culture studies for c-Fms-IN-3 utilize macrophages or other CSF1R-dependent cells. Cells are treated with the compound, and cell viability is assessed using MTT assays. The phosphorylation of CSF1R and its downstream substrates is measured by Western blotting to confirm target inhibition. The effect on macrophage differentiation and function can also be assessed.
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| Animal Protocol |
In vivo animal experiments for c-Fms-IN-3 have been performed in a collagen-induced arthritis mouse model. In this model, the compound is administered, and disease severity is assessed by measuring paw swelling, clinical scores, and histopathological analysis of joints for bone erosion, pannus invasion, and cartilage damage. Inflammatory cytokine levels are measured by ELISA.
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| ADME/Pharmacokinetics |
c-Fms-IN-3 has a molecular formula of C23H30N6O and a molecular weight of 406.52 g/mol. It is a solid compound that is soluble in DMSO (25 mg/mL). It is typically stored as a powder at -20°C (stable for 3 years) or at 4°C (stable for 2 years). In solution, it is stable at -80°C for 6 months and at -20°C for 1 month.
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| Toxicity/Toxicokinetics |
Toxicological data for c-Fms-IN-3 are limited, as it is a research compound. It is not intended for human use. Comprehensive toxicity studies have not been reported. Standard safety precautions for handling chemical reagents should be followed. Its effects on macrophage populations suggest it could have significant immunomodulatory effects.
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| References | |
| Additional Infomation |
4-Cyano-N-[4-(4-methyl-1-piperazinyl)-2-(4-methyl-1-piperidinyl)phenyl]-1H-pyrrole-2-carboxamide is an aromatic amide.
c-Fms-IN-3 is a research compound with no clinical approval. It is a valuable tool for studying CSF1R biology and the role of macrophages in inflammation, cancer, and bone diseases. Its efficacy in the collagen-induced arthritis model makes it a compound of interest for research into rheumatoid arthritis and other inflammatory diseases. |
| Molecular Formula |
C23H30N6O
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|---|---|
| Molecular Weight |
406.5239
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| Exact Mass |
406.248
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| CAS # |
885704-21-2
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| PubChem CID |
11654378
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| Appearance |
White to gray solid powder
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| LogP |
3.267
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
30
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| Complexity |
631
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
DXPSQKSTVIVZLV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H30N6O/c1-17-5-7-29(8-6-17)22-14-19(28-11-9-27(2)10-12-28)3-4-20(22)26-23(30)21-13-18(15-24)16-25-21/h3-4,13-14,16-17,25H,5-12H2,1-2H3,(H,26,30)
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| Chemical Name |
4-cyano-N-[4-(4-methylpiperazin-1-yl)-2-(4-methylpiperidin-1-yl)phenyl]-1H-pyrrole-2-carboxamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~25 mg/mL (~61.50 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.15 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4599 mL | 12.2995 mL | 24.5990 mL | |
| 5 mM | 0.4920 mL | 2.4599 mL | 4.9198 mL | |
| 10 mM | 0.2460 mL | 1.2300 mL | 2.4599 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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