Home Protein Tyrosine Kinase CSF-1R inhibitor - VEGFR inhibitor - c-Kit inhibitor - PDGFR inhibitor Ki20227 For research use only.

Ki20227

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.

Ki20227 Chemical Structure

Ki20227 Chemical Structure

CAS: 623142-96-1

Purity & Quality Control

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

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Biological Activity

Description 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.
Targets
c-Fms [1]
(Cell-free assay)		 VEGFR2 [1]
(Cell-free assay)		 PDGFRβ [1]
(Cell-free assay)		 c-Kit [1]
(Cell-free assay)
2 nM 12 nM 217 nM 451 nM
In vitro
In vitro

Ki20227, a novel quinoline-urea derivative, is a c-Fms tyrosine kinase inhibitor. The IC50s of Ki20227 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. Ki20227 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, Ki20227 inhibits the development of tartrate-resistant acid phosphatase-positive osteoclast-like cells in a dose-dependent manner.[1]
Cell Research Cell lines RAW264.7, M-NFS-60, A375, HUVEC cells
Concentrations 0.1 nM - 3000 nM
Incubation Time 72 h, 1h
Method

M-NFS-60, HUVEC, and A375 cells are seeded on a 96-well culture plate and cultured for 24 hours. Then, culture mediums are changed and incubated for a further 72 hours in the presence or absence of Ki20227 (0.1–3,000 nmol/L).
RAW264.7 cells are serum starved for 12 hours in DMEM containing 0.1% FCS. Serial dilutions of Ki20227 are then added to the cells, and they are incubated for 1 hour. RAW264.7 cells are stimulated with 50 ng/mL of recombinant mouse M-CSF for 4 minutes. c-Fms protein in the RAW264.7 cell lysate is prepared with ice-cold lysis buffer.
In Vivo
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, Ki20227 decreases the number of tartrate-resistant acid phosphatase–positive osteoclast-like cells on bone surfaces in ovariectomized (ovx) rats. These findings suggest that Ki20227 inhibits osteolytic bone destruction through the suppression of M-CSF-induced osteoclast accumulation in vivo.[1]
Animal Research Animal Models Athymic rats (F344/NJcl-rnu), Sprague-Dawley rats
Dosages 20 mg/kg
Administration Oral gavage

Chemical Information & Solubility

Molecular Weight 480.54 Formula

C24H24N4O5S
CAS No. 623142-96-1 SDF --
Smiles CC(C1=NC=CS1)NC(=O)NC2=C(C=C(C=C2)OC3=C4C=C(C(=CC4=NC=C3)OC)OC)OC
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 96 mg/mL ( (199.77 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 3 mg/mL

Water : ˂1 mg/mL


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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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