| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg | |||
| Other Sizes |
| Targets |
c-Fms-IN-1 targets the c-FMS (CSF1R) kinase. It is a potent inhibitor with an IC50 of 0.8 nM. By inhibiting CSF1R, it blocks the signaling pathway downstream of M-CSF, which is crucial for the survival, proliferation, and differentiation of macrophages and osteoclasts. This makes it a valuable tool for studying these cell types.
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| ln Vitro |
In vitro, c-Fms-IN-1 demonstrates potent inhibitory activity against CSF1R. Its IC50 of 0.8 nM indicates high potency. This activity is confirmed in cell-based assays where it inhibits CSF1R-mediated signaling. Its high potency makes it a valuable tool for studying the role of CSF1R in various cell types.
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| ln Vivo |
In vivo, c-Fms-IN-1 is used as a research tool to study the role of CSF1R in various physiological and pathological processes. By inhibiting CSF1R, it can affect macrophage populations, osteoclastogenesis, and tumor-associated macrophages. It is used to explore the therapeutic potential of CSF1R inhibition in cancer, inflammatory diseases, and bone disorders.
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| Enzyme Assay |
The in vitro kinase assay for c-Fms-IN-1 involves measuring its ability to inhibit the phosphorylation activity of CSF1R. The enzyme is incubated with a peptide substrate (SYEGNSYTFIDPTQ) and ATP in the presence of varying concentrations of the compound. The amount of phosphorylated substrate is measured using a fluorescence polarization 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-1 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, survival, and function can also be assessed.
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| Animal Protocol |
In vivo animal experiments for c-Fms-IN-1 are not extensively documented. However, its effects on macrophages and osteoclasts could be studied in relevant disease models. For example, its efficacy in cancer could be tested in xenograft models to study the role of tumor-associated macrophages. Its effects on bone could be studied in models of osteoporosis or arthritis.
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| ADME/Pharmacokinetics |
c-Fms-IN-1 has a molecular formula of C22H27N5O2 and a molecular weight of 393.48 g/mol. It is a solid compound that is soluble in DMSO. It is typically stored as a powder at -20°C for long-term stability. Its stability is maintained under recommended storage conditions. For in vivo studies, it may be formulated in a suitable vehicle.
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| Toxicity/Toxicokinetics |
Toxicological data for c-Fms-IN-1 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 potent CSF1R inhibition suggests it could have significant biological effects.
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| References | |
| Additional Infomation |
c-Fms-IN-1 is a research compound with no clinical approval. It is a valuable tool for studying CSF1R biology and the role of macrophages and osteoclasts in health and disease. Its high potency makes it a valuable tool for target validation and drug discovery programs exploring the therapeutic potential of CSF1R inhibition in cancer, inflammation, and bone diseases.
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| Molecular Formula |
C22H27N5O2
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|---|---|
| Molecular Weight |
393.482084512711
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| Exact Mass |
393.216
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| CAS # |
885703-64-0
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| PubChem CID |
11502871
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.1
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
29
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| Complexity |
606
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N#CC1=CC=C(C(NC2C(N3CCCCC3)=CC(N3CCN(C)CC3)=CC=2)=O)O1
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| InChi Key |
UUPPIQKPNBIUKY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H27N5O2/c1-25-11-13-26(14-12-25)17-5-7-19(20(15-17)27-9-3-2-4-10-27)24-22(28)21-8-6-18(16-23)29-21/h5-8,15H,2-4,9-14H2,1H3,(H,24,28)
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| Chemical Name |
5-cyano-N-[4-(4-methylpiperazin-1-yl)-2-piperidin-1-ylphenyl]furan-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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ~5 mg/mL (~12.71 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.5 mg/mL (1.27 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 5.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.5 mg/mL (1.27 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 5.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5414 mL | 12.7071 mL | 25.4143 mL | |
| 5 mM | 0.5083 mL | 2.5414 mL | 5.0829 mL | |
| 10 mM | 0.2541 mL | 1.2707 mL | 2.5414 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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