| Ki20227C-Fms tyrosine kinase inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- Purity = 98.43%
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Chemical structure
| 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 | ||
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| Cas No. | 623142-96-1 | SDF | Download SDF |
| Synonyms | Ki 20227;Ki-20227 | ||
| Chemical Name | 1-[4-(6,7-dimethoxyquinolin-4-yl)oxy-2-methoxyphenyl]-3-[1-(1,3-thiazol-2-yl)ethyl]urea | ||
| Canonical SMILES | CC(C1=NC=CS1)NC(=O)NC2=C(C=C(C=C2)OC3=C4C=C(C(=CC4=NC=C3)OC)OC)OC | ||
| Formula | C24H24N4O5S | M.Wt | 480.55 |
| Solubility | ≥48.1 mg/mL in DMSO, ≥8.6 mg/mL in EtOH with ultrasonic and warming, <2.22 mg/ml="" in="" h2o=""> | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For 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. | ||
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.
