1-(4-((6,7-Dimethoxyquinolin-4-yl)oxy)-2-methoxyphenyl)-3-(1-(thiazol-2-yl)ethyl)urea
N-[4-[(6,7-Dimethoxy-4-quinolinyl)oxy]-2-methoxyphenyl]-N'-[1-(2-thiazolyl)ethyl]urea
CAS: 623142-96-1
Molecular Formula: C24H24N4O5S
1-(4-((6,7-Dimethoxyquinolin-4-yl)oxy)-2-methoxyphenyl)-3-(1-(thiazol-2-yl)ethyl)urea - Names and Identifiers
| Name | N-[4-[(6,7-Dimethoxy-4-quinolinyl)oxy]-2-methoxyphenyl]-N'-[1-(2-thiazolyl)ethyl]urea |
| Synonyms | KI20227 Ki20227 CS-1094 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]- |
| CAS | 623142-96-1 |
| EINECS | 200-258-5 |
1-(4-((6,7-Dimethoxyquinolin-4-yl)oxy)-2-methoxyphenyl)-3-(1-(thiazol-2-yl)ethyl)urea - Physico-chemical Properties
| Molecular Formula | C24H24N4O5S |
| Molar Mass | 480.54 |
| Density | 1.327 |
| Boling Point | 621.8±55.0 °C(Predicted) |
| Flash Point | 329.846 °C |
| Appearance | Brown powder. |
| pKa | 12.03±0.46(Predicted) |
| Storage Condition | Sealed in dry,Store in freezer, under -20°C |
| In vitro study | Ki20227 (0.1-1000 nM; 72 hours) with 100 and 1,000 nM almost suppresses M-NFS-60 cell growth and HUVEC cell growth, respectively. Ki20227 (0.1-1000 nM; 1 hour) suppresses M-CSF-dependent c-Fms phosphorylation in a dose-dependent manner. Cell Viability Assay Cell Line: M-NFS-60 cells, HUVEC cells, human A375 melanoma cells Concentration: 0.1, 0.3, 1, 3, 10, 30, 100, 300, 1000 nM Incubation Time: 72 hours Result: 100 and 1,000 nM almost suppressed M-NFS-60 cell growth and HUVEC cell growth, respectively. Cell Viability Assay Cell Line: RAW264.7 cell lysate Concentration: 0.1, 0.3, 1, 3, 10, 30, 100, 300, 1000 nM Incubation Time: 1 hour Result: Suppressed M-CSF-dependent c-Fms phosphorylation in a dose-dependent manner. |
| In vivo study | Ki20227 (orally;10-50 mg/kg/d for 20 days) of 50 mg/kg/d of Ki20227 for 20 days markedly decreases the osteolytic lesion areas. ki20227 during global ischemia led to a significant deficit in microglial density in the CNS in mice, and CSF1R-inhibition led to a significant reduction in the neuronal density of mice. Animal Model: 4-week-old male F344/NJcl-rnu rats Dosage: 10, 20, and 50 mg/kg Administration: Orally; once per day for 20 days Result: Oral administration of 50 mg/kg/d markedly decreased the osteolytic lesion areas. |
1-(4-((6,7-Dimethoxyquinolin-4-yl)oxy)-2-methoxyphenyl)-3-(1-(thiazol-2-yl)ethyl)urea - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.081 ml | 10.405 ml | 20.809 ml |
| 5 mM | 0.416 ml | 2.081 ml | 4.162 ml |
| 10 mM | 0.208 ml | 1.04 ml | 2.081 ml |
| 5 mM | 0.042 ml | 0.208 ml | 0.416 ml |
Last Update：2024-01-02 23:10:35
1-(4-((6,7-Dimethoxyquinolin-4-yl)oxy)-2-methoxyphenyl)-3-(1-(thiazol-2-yl)ethyl)urea - Reference Information
| application | N-[4-[(6, 7-dimethoxy-4-quinolyl) oxy]-2-methoxyphenyl]-N'-[1-(2-thiazolyl) ethyl] urea is a c-fms tyrosine kinase inhibitor, it can inhibit osteoclast differentiation and osteolytic bone destruction in bone metastasis models. |
| biological activity | Ki20227 is a highly selective inhibitor of oral active c-Fms tyrosine kinase(CSF1R), the IC50 values 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) are 2 nM, 12 nM, 451 nM, and 217 nM. |
| target | TargetValue 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 |
| Target | Value |
| 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 study | Ki20227 (0.1-1000 nM; 72 hours) with 100 and 1,000 nM once suppresses M-NFS-60 cell growth and HUVEC cell growth, respectively. Ki20227 (0.1-1000 nM; 1 hour) suppresses M-CSF-dependent c-Fms phosphorylation in a dose-dependent manner. Cell Viability Assay Cell Line: M-NFS-60 cells, HUVEC cells, human A375 melanoma cells Concentration: 0.1, 0.3, 1, 3, 10, 30, 100, 300, 1000 nM Incubation Time: 72 hours Result: 100 and 1,000 nM almost suppressed M-NFS-60 cell growth and HUVEC cell growth, respectively. Cell Viability Assay Cell Line: RAW264.7 cell lysate Concentration: 0.1, 0.3, 1, 3, 10, 30, 100, 300, 1000 nM Incubation Time: 1 hour Result: Suppressed M-CSF-dependent c-Fms phosphorylation in a pose-dependent manner. |
| Cell Line: | M-NFS-60 cells, HUVEC cells, human A375 melanoma cells RAW264.7 cell lysate |
| Concentration: | 0.1, 0.3, 1, 3, 10, 30, 100, 300, 1000 nM 0.1, 0.3, 1, 3, 10, 30, 100, 300, 1000 nM |
| Incubation Time: | 72 hours 1 hour |
| Result: | 100 and 1,000 nM almost suppressed M-NFS-60 cell growth and HUVEC cell growth, respectively. Suppressed M-CSF-dependent c-Fms phosphorylation in a dose-dependent manner. Oral administration of 50 mg/kg/d markedly decreased the osteolytic lesion areas. |
| in vivo study | Ki20227 (orally;10-50 mg/kg/d for 20 days) of 50 mg/kg/d of Ki20227 for 20 days markedly decreases the osteolytic lesion areas. ki20227 during global ischemia led to a significant deficit in microglial density in the CNS in mice, and CSF1R-inhibition led to a significant reduction in the neuronal density of mice. Animal Model: 4-week-old male F344/NJcl-rnu rats Dosage: 10, 20, and 50 mg/kg Administration: Orally; Once per day for 20 days result: oral administration of 50 mg/kg/d markedly decreased the osteolytic lesion areas. |
| Animal Model: | 4-week-old male F344/NJcl-rnu rats |
| Dosage: | 10, 20, and 50 mg/kg |
| Administration: | Orally; once per day for 20 days |
Last Update：2024-04-09 19:05:04
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