c-Fms-IN-3
Based on 1 Customer Validation
c-Fms-IN-3 is an orally active c-Fms (CSF1R) kinase inhibitor (IC50 = 0. 8 nM). c-Fms-IN-3 inhibits CSF1R kinase activity and reduces macrophage populations. c-Fms-IN-3 reduces bone erosion, pannus invasion, cartilage damage, and inflammation in collagen (HY-NP003)-induced arthritis mouse model. c-Fms-IN-3 is useful for arthritis research.
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- Purity : 98.87%
- CAS No.: 885704-21-2
- 화학식: C23H30N6O
- 분자량:406.52
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
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Biological Activity
제품 설명
IC50 & Target
c-Fms.
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Sf9 | IC50 |
0.00078 μM
Compound: 8
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Inhibition of human cytoplasmic FMS expressed in Sf9-baculovirus system after 80 mins by fluorescence polarization
Inhibition of human cytoplasmic FMS expressed in Sf9-baculovirus system after 80 mins by fluorescence polarization
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[PMID: 18242992] |
| Sf9 | IC50 |
0.78 nM
Compound: 8
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Inhibition of human cytoplasmic FMS expressed in Sf9-baculovirus system after 80 mins by fluorescence polarization
Inhibition of human cytoplasmic FMS expressed in Sf9-baculovirus system after 80 mins by fluorescence polarization
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[PMID: 18242992] |
In Vitro
Parmacokinetics
| Species | Dose | Route | T1/2 | Cmax | Vss | CL | F |
|---|---|---|---|---|---|---|---|
| Mice[1] | 10 mg/kg | p.o. | 244 min | 853 ng/mL | 5635 mL/kg | 16 | 45 % |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Murine collagen-induced model of arthritis (CIA)[1]
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Dosage:30 and 5 mg/kg
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Administration:p.o., twice-daily, 14 days
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Result:Reduced pannus formation and the destruction of bone and cartilage, reduced pannus growth and bone destruction by 80%.
Depleted macrophages, demonstrated that macrophages are the target.
Chemical Information
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CAS No. 885704-21-2
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Appearance Solid
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분자량 406.52
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화학식 C23H30N6O
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Color White to gray
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SMILES
CN(CC1)CCN1C2=CC=C(NC(C3=CC(C#N)=CN3)=O)C(N4CCC(C)CC4)=C2
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
용액&용해도
In Vitro:
DMSO : 25 mg/mL (61.50 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (275 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Illig, Carl R.; Chen, Jinsheng; Wall, Mark J. et al. Discovery of novel FMS kinase inhibitors as anti-inflammatory agents. Bioorganic & Medicinal Chemistry Letters (2008), 18(5), 1642-1648. [Content Brief]
[2]. Meegalla, Sanath K.; Wall, Mark J.; Chen, Jinsheng et al. Structure-based optimization of a potent class of arylamide FMS inhibitors. Bioorganic & Medicinal Chemistry Letters (2008), 18(12), 3632-3637. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4599 mL | 12.2995 mL | 24.5990 mL | 61.4976 mL |
| 5 mM | 0.4920 mL | 2.4599 mL | 4.9198 mL | 12.2995 mL | |
| 10 mM | 0.2460 mL | 1.2300 mL | 2.4599 mL | 6.1498 mL | |
| 15 mM | 0.1640 mL | 0.8200 mL | 1.6399 mL | 4.0998 mL | |
| 20 mM | 0.1230 mL | 0.6150 mL | 1.2300 mL | 3.0749 mL | |
| 25 mM | 0.0984 mL | 0.4920 mL | 0.9840 mL | 2.4599 mL | |
| 30 mM | 0.0820 mL | 0.4100 mL | 0.8200 mL | 2.0499 mL | |
| 40 mM | 0.0615 mL | 0.3075 mL | 0.6150 mL | 1.5374 mL | |
| 50 mM | 0.0492 mL | 0.2460 mL | 0.4920 mL | 1.2300 mL | |
| 60 mM | 0.0410 mL | 0.2050 mL | 0.4100 mL | 1.0250 mL |
c-Fms-IN-3 Related Classifications
HY-13075 Related Classifications
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