2. Protein Tyrosine Kinase/RTK
  3. c-Fms VEGFR c-Kit PDGFR
  4. Ki20227

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.

For research use only. We do not sell to patients.

Ki20227 Chemical Structure

Ki20227 Chemical Structure

CAS No. : 623142-96-1

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10 mM * 1 mL in DMSO
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Customer Review

Based on 5 publication(s) in Google Scholar

Ki20227 Related Antibodies

Top Publications Citing Use of Products

View All VEGFR Isoform Specific Products:

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VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

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PDGFR PDGFRβ PDGFRα

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

IC50 & Target

IC50: 2 nM (CSF1R), 12 nM (VEGFR2), 451 nM (c-Kit) and 217 nM (PDGFRβ)[1]
Cellular Effect
Cell Line Type Value Description References
BaF3 EC50
76 nM
Compound: 6; KI20227
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
[PMID: 34606263]
NFS-60 EC50
77 nM
Compound: 6; KI20227
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
[PMID: 34606263]
In Vitro

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.

Ki20227 Related Antibodies

Cell Viability Assay[1]

Cell Line: M-NFS-60 cells, HUVEC cells, human A375 melanoma cells
Concentration: 0.1, 0.3, 1, 3, 10, 30, 100, 300, 1000 nM
Incubation Time: 72 hours
Result: 100 and 1,000 nM almost suppressed M-NFS-60 cell growth and HUVEC cell growth, respectively.

Cell Viability Assay[1]

Cell Line: RAW264.7 cell lysate
Concentration: 0.1, 0.3, 1, 3, 10, 30, 100, 300, 1000 nM
Incubation Time: 1 hour
Result: Suppressed M-CSF-dependent c-Fms phosphorylation in a dose-dependent manner.
In Vivo

Ki20227 (orally;10-50 mg/kg/d for 20 days) of 50 mg/kg/d of Ki20227 for 20 days markedly decreases the osteolytic lesion areas[1].
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.

Animal Model: 4-week-old male F344/NJcl-rnu rats[1]
Dosage: 10, 20, and 50 mg/kg
Administration: Orally; once per day for 20 days
Result: Oral administration of 50 mg/kg/d markedly decreased the osteolytic lesion areas.
Molecular Weight

480.54

Formula

C24H24N4O5S
CAS No.
Appearance

Solid

Color

Off-white to pink

SMILES

O=C(NC1=CC=C(C=C1OC)OC2=CC=NC3=CC(OC)=C(C=C23)OC)NC(C)C4=NC=CS4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (130.06 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0810 mL 10.4050 mL 20.8099 mL
5 mM 0.4162 mL 2.0810 mL 4.1620 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

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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Ki20227 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ki20227623142-96-1Ki 20227Ki-20227c-FmsVEGFRc-KitPDGFRCSF-1 receptorcolony stimulating factor 1 receptorCSF-1RCSF1RVascular endothelial growth factor receptorSCFRCD117Platelet-derived growth factor receptorInhibitorinhibitorinhibit

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