| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg | |||
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| Targets |
c-Fms-IN-8 targets the colony-stimulating factor-1 receptor (CSF-1R, also known as c-FMS), a type III receptor tyrosine kinase. CSF-1R is activated by its ligands, colony-stimulating factor-1 (CSF-1) and interleukin-34 (IL-34), and plays critical roles in the survival, proliferation, and differentiation of macrophages, osteoclasts, and other myeloid cells. CSF-1R signaling is involved in various physiological and pathological processes, including inflammation, bone remodeling, and tumor progression. By inhibiting CSF-1R, c-Fms-IN-8 blocks downstream signaling pathways and modulates macrophage function. The compound is a Type II inhibitor, which binds to the inactive conformation of the kinase.
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| ln Vitro |
c-Fms-IN-8 demonstrates potent in vitro activity as a CSF-1R inhibitor. The compound has an IC50 of 9.1 nM against CSF-1R. Its activity is concentration-dependent, with potent inhibition observed at nanomolar concentrations. c-Fms-IN-8 is a Type II inhibitor of CSF-1R. The compound's potency and selectivity make it a valuable tool for studying CSF-1R biology and evaluating CSF-1R inhibition as a therapeutic strategy for diseases involving macrophages, such as cancer, inflammation, and bone disorders. The compound's in vitro activity has been characterized in kinase assays and cell-based systems.
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| ln Vivo |
In vivo, c-Fms-IN-8 has been studied for its potential in diseases involving CSF-1R signaling, such as cancer, inflammation, and bone disorders. As a potent CSF-1R inhibitor, the compound modulates macrophage function and has potential therapeutic applications. Comprehensive in vivo efficacy data for c-Fms-IN-8 have been reported in research publications. The compound's ability to inhibit CSF-1R in vivo supports its use in preclinical studies. Its pharmacokinetic properties support its use in animal models. The compound's effects on macrophage-mediated processes are of particular interest.
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| Enzyme Assay |
In vitro kinase assays for c-Fms-IN-8 involve measuring the inhibition of CSF-1R kinase activity. Recombinant CSF-1R kinase is incubated with varying concentrations of the test compound, ATP, and a peptide substrate. The transfer of the phosphate group from ATP to the substrate is quantified using radioactive [33P]-ATP or by detecting phosphorylated peptide using a luminescent method such as the ADP-Glo assay. IC50 values are calculated by plotting percent inhibition against compound concentration using non-linear regression analysis. The compound has an IC50 of 9.1 nM against CSF-1R. Selectivity assays compare the compound's activity against a panel of other kinases. Each concentration is typically tested in duplicate or triplicate.
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| Cell Assay |
In vitro cellular assays for c-Fms-IN-8 are performed using cell lines that express CSF-1R, such as macrophages or CSF-1R-transfected cells. Cells are treated with varying concentrations of the compound for defined time periods. CSF-1R phosphorylation and downstream signaling (e.g., ERK, AKT) are assessed by Western blot using phospho-specific antibodies. Cell proliferation and survival are measured using MTT or CellTiter-Glo assays. Macrophage differentiation and function can be assessed using appropriate assays. Cytotoxicity is assessed in parallel using standard viability assays to ensure that observed effects are not due to cell death. IC50 values for inhibition of CSF-1R phosphorylation or cell proliferation are calculated from dose-response curves.
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| Animal Protocol |
In vivo animal studies for c-Fms-IN-8 are conducted using rodent models of cancer, inflammation, and bone disorders. The compound is administered via oral gavage, intraperitoneal injection, or subcutaneous injection at various doses and schedules. In cancer models, tumor-bearing mice are treated with c-Fms-IN-8, and tumor growth is measured using calipers. Macrophage infiltration into tumors is assessed by immunohistochemistry or flow cytometry. In inflammatory disease models, inflammatory parameters are assessed. In bone disorder models, bone resorption and osteoclast numbers are assessed. Pharmacokinetic studies assess drug concentrations in plasma and tissues. Animals are monitored for clinical signs and body weight. Efficacy is expressed as tumor growth inhibition or improvement in disease parameters compared to vehicle-treated controls.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of c-Fms-IN-8 have been characterized in preclinical studies. The compound has a molecular formula of C27H30N2O5 and a molecular weight of 462.54 g/mol. Its chemical name is 2-{[2-(3-{4-[(4-ethylphenyl)methoxy]-3-methoxyphenyl}azetidine-1-carbonyl)pyridin-4-yl]oxy}ethan-1-ol. Comprehensive pharmacokinetic parameters including half-life, volume of distribution, clearance, and oral bioavailability have been characterized in animal models. The compound's pharmacokinetic profile supports its use in preclinical studies of CSF-1R-related diseases. Detailed pharmacokinetic data are available from research publications.
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| Toxicity/Toxicokinetics |
c-Fms-IN-8 is intended for laboratory research use only and has not undergone comprehensive clinical toxicology testing. As a CSF-1R inhibitor that modulates macrophage function, the compound would be expected to have effects on immune function and inflammation. Standard in vitro cytotoxicity assays in cell lines are typically performed alongside efficacy studies to rule out nonspecific toxicity. In vivo, animals are monitored for signs of toxicity including body weight changes, behavioral abnormalities, and clinical observations. Comprehensive toxicological characterization including genotoxicity and repeated-dose toxicity studies has been conducted as part of preclinical development. The compound is not approved for human use and is strictly intended for research purposes.
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| References | |
| Additional Infomation |
c-Fms-IN-8 is a potent Type II inhibitor of CSF-1R (c-FMS) with an IC50 of 9.1 nM. It has a molecular formula of C27H30N2O5 and a molecular weight of 462.54 g/mol. c-Fms-IN-8 is compound 4a in the reference literature. The compound has not entered clinical trials and has not received regulatory approval for any indication. It is available from research chemical suppliers for non-clinical research purposes only. c-Fms-IN-8 is a valuable research tool for studying CSF-1R biology and developing new therapies for cancer, inflammation, and bone disorders.
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| Molecular Formula |
C27H30N2O5
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| Molecular Weight |
462.54
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| Exact Mass |
462.215
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| CAS # |
1255303-58-2
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| PubChem CID |
59634061
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| Appearance |
White to off-white solid powder
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| LogP |
3.7
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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 |
10
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| Heavy Atom Count |
34
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| Complexity |
620
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1(=CC(=CC=N1)OCCO)C(N1CC(C2=CC(=C(C=C2)OCC2=CC=C(C=C2)CC)OC)C1)=O
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| InChi Key |
KVXLTGRHKNTTMZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H30N2O5/c1-3-19-4-6-20(7-5-19)18-34-25-9-8-21(14-26(25)32-2)22-16-29(17-22)27(31)24-15-23(10-11-28-24)33-13-12-30/h4-11,14-15,22,30H,3,12-13,16-18H2,1-2H3
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| Chemical Name |
[3-[4-[(4-ethylphenyl)methoxy]-3-methoxyphenyl]azetidin-1-yl]-[4-(2-hydroxyethoxy)pyridin-2-yl]methanone
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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: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ~100 mg/mL (~216.20 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.40 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 | 2.1620 mL | 10.8099 mL | 21.6198 mL | |
| 5 mM | 0.4324 mL | 2.1620 mL | 4.3240 mL | |
| 10 mM | 0.2162 mL | 1.0810 mL | 2.1620 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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