Toggle Nav

Ki20227

In stock
Catalog No.
A3527
C-Fms tyrosine kinase inhibitor
Grouped product items
SizePriceStock Qty
10mg
$205.00
In stock
50mg
$822.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

The IC50s of Ki20227 inhibiting c-Fms, stem cell factor receptor (c-Kit), vascular endothelial growth factor receptor-2 (KDR), and platelet-derived growth factor receptor B were found to be 2, 451, 12, and 217 nmol/L, respectively.

Macrophage colony-stimulating factor (M-CSF) is required for the development of individual mononuclear phagocyte populations and is involved in the immune response. Ki20227 (N-{4-[(6,7-dimethoxy-4-quinolyl)-oxy]-2-methoxyphenyl}-N'-[1-(1,3-thiazole-2-yl)ethyl] urea) is a highly selective M-CSF receptor (c-fms) tyrosine kinase inhibitor.

In vitro: Ki20227 was found to inhibit c-Fms, KDR, c-Kit, and platelet-derived growth factor receptor B, but not inhibit other kinases tested, such as epidermal growth factor receptor, fms-like tyrosine kinase-3 , or c-Src. Ki20227 was also found to inhibit the M-CSF dependent growth of M-NFS-60 cells but not the M-CSF independent growth of A375 human melanoma cells. Furthermore, Ki20227 inhibited the development of tartrate-resistant acid phosphatase-positive osteoclast-like cells in a dose-dependent manner [1].

In vivo: Oral administration of Ki20227 suppressed osteoclast-like cell accumulation and bone resorption induced by metastatic tumor cells in nude rats following intracardiac injection of A375 cells. In addition, Ki20227 decreased the number of tartrate-resistant acid phosphatase-positive osteoclast-like cells on bone surfaces in ovariectomized (ovx) rats [1].

Clinical trial: Ki20227 is currently in the preclinical developlent stage and no clinical data are available.

Reference:
[1] Ohno H, Kubo K, Murooka H, Kobayashi Y, Nishitoba T, Shibuya M, Yoneda T, Isoe T.   A c-fms tyrosine kinase inhibitor, Ki20227, suppresses osteoclast differentiation and osteolytic bone destruction in a bone metastasis model. Mol Cancer Ther. 2006;5(11):2634-43.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt480.55
Cas No.623142-96-1
FormulaC24H24N4O5S
SynonymsKi 20227;Ki-20227
Solubility≥48.1 mg/mL in DMSO, ≥8.6 mg/mL in EtOH with ultrasonic and warming, <2.22 mg/mL in H2O
Chemical Name1-[4-(6,7-dimethoxyquinolin-4-yl)oxy-2-methoxyphenyl]-3-[1-(1,3-thiazol-2-yl)ethyl]urea
SDFDownload SDF
Canonical SMILESCC(C1=NC=CS1)NC(=O)NC2=C(C=C(C=C2)OC3=C4C=C(C(=CC4=NC=C3)OC)OC)OC
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Description Ki20227 is a highly selective inhibitor of c-Fms tyrosine kinase with IC50 value of 2 nM.
Targets c-Fms VEGFR-2 PDGFRβ c-Kit    
IC50 2 nM 12 nM 217 nM 451 nM    

Quality Control

Chemical structure

Ki20227