Cat. No.: HY-10408

Ki20227

4 Cited Publications

Customer Review

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.

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

Purity: 99.51%
CAS No.: 623142-96-1
Formula: C₂₄H₂₄N₄O₅S
Molecular Weight:480.54

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Ki20227 Chemical Structure

CAS No.: 623142-96-1

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (4)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

IC50: 2 nM (CSF1R), 12 nM (VEGFR2), 451 nM (c-Kit) and 217 nM (PDGFRβ)^[1]

All VEGFR Isoforms :

All PDGFR Isoforms :

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.

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.

Chemical Information

CAS No. 623142-96-1
Appearance Solid
Molecular Weight 480.54
Formula C₂₄H₂₄N₄O₅S
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

Publications (4)

All IFIn Vivo Efficacy StudyHistological Imaging/StainingWBRT-PCR

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Journal Impact Factor

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.).
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
Int J Clin Exp Pathol

2016;9(12):12459-12469.

Solvent & Solubility

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0810 mL

10.4050 mL

20.8099 mL

5 mM

0.4162 mL

2.0810 mL

4.1620 mL

10 mM

0.2081 mL

1.0405 mL

2.0810 mL

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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

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Volume _(start) Volume _(start)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.17 mg/mL (4.52 mM); Clear solution

This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Ohno H, et al. A c-fms tyrosine kinase inhibitor, Ki20227, suppresses osteoclast differentiation and osteolytic bone destruction in a bone metastasis model. Mol Cancer Ther. 2006 Nov;5(11):2634-43. [Content Brief]

[2]. Boru Hou, et al. Ki20227 influences the morphology of microglia and neurons through inhibition of CSF1R during global ischemia. Int J Clin Exp Pathol. 2016;9(12):12459-12469.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Coagulation and Anti-coagulation Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Macrophage Related Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Ki20227

All VEGFR Isoforms

All PDGFR Isoforms

Biological Activity

Chemical Information

Publications (4)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Ki20227 Related Classifications

HY-10408 Related Classifications