Ki20227
Based on 4 publication(s) in Google Scholar
Ki20227 is an orally active and highly selective c-Fms tyrosine kinase (CSF1R) inhibitor with IC50s of 2 nM, 12 nM, 451 and 217 nM for CSF1R, VEGFR2 (vascular endothelial growth factor receptor-2), c-Kit (stem cell factor receptor) and PDGFRβ (platelet-derived growth factor receptor β). Ki20227 suppresses osteoclast differentiation and osteolytic bone destruction.
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- Pureté: 99.51%
- CAS No.: 623142-96-1
- Formule: C24H24N4O5S
- Masse moléculaire:480.54
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Stockage: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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Ki20227
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IF
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In Vivo Efficacy Study
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Histological Imaging/Staining
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Activité biologique
IC50: 2 nM (CSF1R), 12 nM (VEGFR2), 451 nM (c-Kit) and 217 nM (PDGFRβ)[1]
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Cell Line
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Type | Value | Description | References |
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| BaF3 | EC50 |
76 nM
Compound: 6; KI20227
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Antiproliferative activity against mouse BaF3 cells transfected with human ETV6-CSF1R assessed as reduction in cell viability measured after 72 hrs by MTS method
Antiproliferative activity against mouse BaF3 cells transfected with human ETV6-CSF1R assessed as reduction in cell viability measured after 72 hrs by MTS method
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[PMID: 34606263] |
| NFS-60 | EC50 |
77 nM
Compound: 6; KI20227
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Antiproliferative activity against mouse NFS-60 cells transfected with human ETV6-CSF1R assessed as reduction in cell viability measured after 72 hrs by MTS method
Antiproliferative activity against mouse NFS-60 cells transfected with human ETV6-CSF1R assessed as reduction in cell viability measured after 72 hrs by MTS method
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[PMID: 34606263] |
Ki20227 (0.1-1000 nM; 72 hours) with 100 and 1,000 nM almost suppresses M-NFS-60 cell growth and HUVEC cell growth, respectively[1].
Ki20227 (0.1-1000 nM; 1 hour) suppresses M-CSF-dependent c-Fms phosphorylation in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:M-NFS-60 cells, HUVEC cells, human A375 melanoma cells
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Concentration:0.1, 0.3, 1, 3, 10, 30, 100, 300, 1000 nM
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Incubation Time:72 hours
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Result:100 and 1,000 nM almost suppressed M-NFS-60 cell growth and HUVEC cell growth, respectively.
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Cell Line:RAW264.7 cell lysate
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Concentration:0.1, 0.3, 1, 3, 10, 30, 100, 300, 1000 nM
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Incubation Time:1 hour
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Result:Suppressed M-CSF-dependent c-Fms phosphorylation in a dose-dependent manner.
ki20227 during global ischemia led to a significant deficit in microglial density in the CNS in mice, and CSF1R-inhibition led to a significant reduction in the neuronal density of mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:4-week-old male F344/NJcl-rnu rats[1]
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Dosage:10, 20, and 50 mg/kg
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Administration:Orally; once per day for 20 days
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Result:Oral administration of 50 mg/kg/d markedly decreased the osteolytic lesion areas.
Chemical Information
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CAS No. 623142-96-1
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Appearance Solid
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Masse moléculaire 480.54
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Formule C24H24N4O5S
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Color Off-white to pink
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SMILES
O=C(NC1=CC=C(C=C1OC)OC2=CC=NC3=CC(OC)=C(C=C23)OC)NC(C)C4=NC=CS4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Neural Regen Res
Ki20227 aggravates apoptosis, inflammatory response, and oxidative stress after focal cerebral ischemia injury. [Abstract]2022 Jan;17(1):137-143. PMID: 34100449
Ki20227 purchased from MedChemExpress. Usage Cited in: Neural Regen Res. 2022 Jan;17(1):137-143. [Abstract]
Representative confocal images of Iba1-positive (green, stained by fluorescein isothiocyanate) microglia and BrdU-positive (red, stained by tetramethylrhodamine) cells in the peri-infarct region treated with Ki20227 (3 mg/g, p.o.).
Ki20227 purchased from MedChemExpress. Usage Cited in: Neural Regen Res. 2022 Jan;17(1):137-143. [Abstract]
Representative infarct volume images following TTC staining. No infarct was observed in the sham groups. Larger infarct volumes were observed in the tMCAO + Ki20227 (3 mg/g, p.o.) group than tMCAO + vehicle group.
Ki20227 purchased from MedChemExpress. Usage Cited in: Neural Regen Res. 2022 Jan;17(1):137-143. [Abstract]
Representative Nissl staining images in the peri-infarct region. Fewer peri-infarct Nissl bodies (arrows) were observed in the tMCAO + Ki20227 (3 mg/g, p.o.) group than in the tMCAO + vehicle group.
Ki20227 purchased from MedChemExpress. Usage Cited in: Neural Regen Res. 2022 Jan;17(1):137-143. [Abstract]
Western blot analysis of Bcl-2, Bax, and Cleaved caspase-3 treated with Ki20227 (3 mg/g, p.o.).
Ki20227 purchased from MedChemExpress. Usage Cited in: Neural Regen Res. 2022 Jan;17(1):137-143. [Abstract]
Quantitative polymerase chain reaction analysis of the mRNA expression levels of CSF1R, IL-6, IL-1β, TNF-α and iNOS treated with Ki20227 (3 mg/g, p.o.).
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Brain Behav Immun
Suppression of microglial activation and monocyte infiltration ameliorates cerebellar hemorrhage induced-brain injury and ataxia. [Abstract]2020 Oct;89:400-413. PMID: 32717406 -
Cell Signal
LncRNA-HOXC-AS2 regulates tumor-associated macrophage polarization through the STAT1/SOCS1 and STAT1/CIITA pathways to promote the progression of non-small cell lung cancer. [Abstract]2024 Mar:115:111031. PMID: 38168631 -
Solvant et solubilité
DMSO : 58.33 mg/mL (121.38 mM; ultrasonic and warming and heat to 60°C; 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)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.17 mg/mL (4.52 mM); Clear solution
This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.17 mg/mL (4.52 mM); Clear solution
This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Pureté et documentation
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Fiche technique (283 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Instruction de manipulation (2659 KB)
Références
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 | 2.0810 mL | 10.4050 mL | 20.8099 mL | 52.0248 mL |
| 5 mM | 0.4162 mL | 2.0810 mL | 4.1620 mL | 10.4050 mL | |
| 10 mM | 0.2081 mL | 1.0405 mL | 2.0810 mL | 5.2025 mL | |
| 15 mM | 0.1387 mL | 0.6937 mL | 1.3873 mL | 3.4683 mL | |
| 20 mM | 0.1040 mL | 0.5202 mL | 1.0405 mL | 2.6012 mL | |
| 25 mM | 0.0832 mL | 0.4162 mL | 0.8324 mL | 2.0810 mL | |
| 30 mM | 0.0694 mL | 0.3468 mL | 0.6937 mL | 1.7342 mL | |
| 40 mM | 0.0520 mL | 0.2601 mL | 0.5202 mL | 1.3006 mL | |
| 50 mM | 0.0416 mL | 0.2081 mL | 0.4162 mL | 1.0405 mL | |
| 60 mM | 0.0347 mL | 0.1734 mL | 0.3468 mL | 0.8671 mL | |
| 80 mM | 0.0260 mL | 0.1301 mL | 0.2601 mL | 0.6503 mL | |
| 100 mM | 0.0208 mL | 0.1040 mL | 0.2081 mL | 0.5202 mL |
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