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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
IC50: 0.017 μM (cFMS)[1]
cFMS Receptor Inhibitor IV targets the cFMS receptor, also known as CSF-1R (colony-stimulating factor 1 receptor). It is an ATP-competitive inhibitor that exhibits inhibitory activity on ATP-induced autophosphorylation of cFMS tyrosine kinase. By blocking the kinase activity of cFMS, it prevents the downstream signaling that promotes the survival, proliferation, and function of macrophages. This makes it a potential therapeutic target for diseases driven by macrophage activation. |
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| ln Vitro |
In vitro, cFMS Receptor Inhibitor IV is a potent inhibitor of cFMS with an IC50 of 0.017 μM (17 nM). It is a cell-permeable compound that acts by competing with ATP for binding to the kinase domain. Its activity is assessed using biochemical kinase assays that measure the phosphorylation of a substrate in the presence of varying concentrations of the inhibitor.
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| ln Vivo |
In vivo activity of cFMS Receptor Inhibitor IV is not extensively documented in the available literature. As a potent CSF-1R inhibitor, its efficacy would be evaluated in animal models of inflammatory diseases and cancer. By blocking cFMS receptor signaling, the inhibitor aims to modulate immune responses and reduce inflammation. Such studies would involve administering the compound and monitoring disease progression.
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| Enzyme Assay |
Cell-free assays for cFMS Receptor Inhibitor IV typically involve measuring its inhibitory activity against cFMS kinase using a biochemical kinase assay. The IC50 value of 0.017 μM is determined by measuring the phosphorylation of a peptide substrate in the presence of varying concentrations of the inhibitor. These assays are used to characterize the compound's potency and mechanism of action as an ATP-competitive inhibitor.
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| Cell Assay |
In vitro cellular assays are conducted to evaluate the functional activity of cFMS Receptor Inhibitor IV. Macrophage cell lines are treated with the compound, and CSF-1R phosphorylation and downstream signaling are measured to assess inhibition. Cell survival and proliferation assays may be used to evaluate the compound's effects on macrophage populations. These assays confirm that the compound effectively blocks CSF-1R-mediated signaling.
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| Animal Protocol |
In vivo animal experiments are not typically detailed for cFMS Receptor Inhibitor IV in the available literature. However, to study its in vivo efficacy, researchers would use animal models of inflammatory diseases or cancer. Animals would be administered the compound, and disease progression, inflammation, or macrophage populations would be monitored to assess its therapeutic potential.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of cFMS Receptor Inhibitor IV are typical of a small molecule inhibitor. Its molecular weight is 378.47. The compound is cell-permeable and is soluble in DMSO. While detailed PK parameters are not widely published, its properties suggest it is designed to have favorable drug-like characteristics to support efficacy in vivo.
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| Toxicity/Toxicokinetics |
The toxicity profile of cFMS Receptor Inhibitor IV is not extensively documented. As a research compound, standard safety precautions should be taken when handling it. Its use is restricted to research purposes and it is not intended for human consumption. Preclinical studies would be required to fully assess its safety profile.
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| References | |
| Additional Infomation |
cFMS Receptor Inhibitor IV is a research compound that targets the cFMS/CSF-1R receptor. Its potent inhibitory activity (IC50 = 17 nM) and cell-permeable nature make it a valuable tool for studying the role of CSF-1R in macrophage biology, inflammation, and cancer. The compound is not approved for therapeutic use.
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| Molecular Formula |
C22H26N4O2
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|---|---|
| Molecular Weight |
378.47
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| Exact Mass |
378.206
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| CAS # |
959626-45-0
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| PubChem CID |
28408236
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.26g/cm3
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| Boiling Point |
530.5ºC at 760 mmHg
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| Flash Point |
274.6ºC
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| Index of Refraction |
1.63
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| LogP |
4.587
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
28
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| Complexity |
576
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CCN(CC1)C2=CC(=C(C=C2)N3CCCCC3)NC(=O)C4=CC=C(O4)C#N
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| InChi Key |
FQGXFVDABCBEFW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H26N4O2/c23-16-18-8-10-21(28-18)22(27)24-19-15-17(25-11-3-1-4-12-25)7-9-20(19)26-13-5-2-6-14-26/h7-10,15H,1-6,11-14H2,(H,24,27)
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| Chemical Name |
5-cyano-N-[2,5-di(piperidin-1-yl)phenyl]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: 31.25 mg/mL (82.57 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6422 mL | 13.2111 mL | 26.4222 mL | |
| 5 mM | 0.5284 mL | 2.6422 mL | 5.2844 mL | |
| 10 mM | 0.2642 mL | 1.3211 mL | 2.6422 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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