| Identification | Back Directory | [Name]
N-[4-[(6,7-Dimethoxy-4-quinolinyl)oxy]-2-methoxyphenyl]-N'-[1-(2-thiazolyl)ethyl]urea | [CAS]
623142-96-1 | [Synonyms]
Ki20227
CS-1094
KI20227; KI 20227
KI20227; KI-20227; KI 20227
N-[4-[(6,7-Dimethoxy-4-quinolinyl)oxy]-2-methoxyphenyl]-N'-[1-(2-thiazolyl)ethyl]urea
1-(4-((6,7-Dimethoxyquinolin-4-yl)oxy)-2-methoxyphenyl)-3-(1-(thiazol-2-yl)ethyl)urea
1-[4-(6,7-dimethoxyquinolin-4-yl)oxy-2-methoxyphenyl]-3-[1-(1,3-thiazol-2-yl)ethyl]urea
Urea, N-[4-[(6,7-diMethoxy-4-quinolinyl)oxy]-2-Methoxyphenyl]-N'-[1-(2-thiazolyl)ethyl]- | [EINECS(EC#)]
200-258-5 | [Molecular Formula]
C24H24N4O5S | [MDL Number]
MFCD12024693 | [MOL File]
623142-96-1.mol | [Molecular Weight]
480.54 |
| Chemical Properties | Back Directory | [Boiling point ]
621.8±55.0 °C(Predicted) | [density ]
1.327 | [storage temp. ]
Sealed in dry,Store in freezer, under -20°C | [solubility ]
≥48.1 mg/mL in DMSO; insoluble in H2O; ≥8.6 mg/mL in EtOH with gentle warming and ultrasonic | [form ]
Brown powder. | [pka]
12.03±0.46(Predicted) |
| Hazard Information | Back Directory | [Description]
Ki20227 is an inhibitor of macrophage colony stimulating factor 1 (CSF1) receptor tyrosine kinase (c-Fms; IC50 = 2 nM).1 It inhibits CSF1-dependent c-Fms phosphorylation in a dose-dependent manner in RAW264.7 cells and reduces CSF1-dependent growth of M-NFS-60 cells (IC50 = 14 nM). Ki20227 suppresses development of TRAP-positive osteoclast-like cells from murine bone marrow (IC50 = 40 nM) and decreases the number and area of osteolytic lesions on femurs and tibiae in a murine A375 subcutaneous xenograft model. Ki20227 also reduces TNF-α infiltration and osteolytic bone destruction in a collagen-induced arthritis (CIA) mouse model.2 | [Uses]
Ki 20227 is a c-fms tyrosine kinase inhibitor, which suppresses osteoclast differentiation and osteolytic bone destruction in a bone metastasis model. | [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]. | [storage]
Store at +4°C | [References]
[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. |
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