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Ki20227 CSF-1R inhibitor

Name: Ki20227
Brand: Selleck Chemicals
SKU: S7688
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S7688

Ki20227 is an orally active and highly selective inhibitor of c-Fms tyrosine kinase(CSF1R) with IC50 of 2 nM, 12 nM, 451 nM and 217 nM for c-Fms, vascular endothelial growth factor receptor-2 (KDR/VEGFR-2), stem cell factor receptor (c-Kit), and platelet-derived growth factor receptor beta (PDGFRβ), respectively.

Chemical Structure

Molecular Weight: 480.54

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Quality Control

Batch: S768801 DMSO]96 mg/mL]false]Ethanol]3 mg/mL]false]Water]˂1 mg/mL]false Purity: 99.40%

Cited in Nature Medicine for its top-tier quality
COA
HPLC
SDS
Datasheet

99.40

Related Targets	EGFR VEGFR PDGFR FGFR c-Met Src MEK FLT3 HER2 c-Kit
Other CSF-1R Inhibitors	Sotuletinib (BLZ945) GW2580 PLX5622 Edicotinib(JNJ-40346527) CSF1R-IN-1 Sulfatinib Vimseltinib AZD7507 Chiauranib ARRY-382

Solubility

In vitro
Batch:

DMSO : 96 mg/mL (199.77 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 3 mg/mL

Water : ˂1 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.600mg/ml (1.25mM)	Taking the 1 mL working solution as an example, add 50 μL of 12 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.600mg/ml (1.25mM)	Taking the 1 mL working solution as an example, add 50 μL of 12 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	480.54	Formula	C₂₄H₂₄N₄O₅S	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	623142-96-1	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Mechanism of Action

Targets/IC₅₀/Ki	c-Fms (Cell-free assay) 2 nM VEGFR2 (Cell-free assay) 12 nM PDGFRβ (Cell-free assay) 217 nM c-Kit (Cell-free assay) 451 nM
In vitro	Ki20227, a novel quinoline-urea derivative, is a c-Fms tyrosine kinase inhibitor. The IC50s of this compound to inhibit c-Fms, vascular endothelial growth factor receptor-2 (KDR), stem cell factor receptor (c-Kit), and platelet-derived growth factor receptor B are found to be 2, 12, 451, and 217 nmol/L, respectively. It is also found to inhibit the M-CSFdependent growth of M-NFS-60 cells but not the M-CSFindependent growth of A375 human melanoma cells in vitro. Furthermore, in an osteoclast-like cell formation assay using mouse bone marrow cells, this chemical inhibits the development of tartrate-resistant acid phosphatase-positive osteoclast-like cells in a dose-dependent manner.
In vivo	In in vivo studies, oral administration of Ki20227 suppresses osteoclast-like cell accumulation and bone resorption induced by metastatic tumor cells in nude rats following intracardiac injection of A375 cells. Moreover, this compound decreases the number of tartrate-resistant acid phosphatase–positive osteoclast-like cells on bone surfaces in ovariectomized (ovx) rats. These findings suggest that this chemical inhibits osteolytic bone destruction through the suppression of M-CSF-induced osteoclast accumulation in vivo.
References	[1] https://pubmed.ncbi.nlm.nih.gov/17121910/

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