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623142-96-1

中文名称 N-[4-[(6,7-二甲氧基-4-喹啉基)氧基]-2-甲氧基苯基]-N'-[1-(2-噻唑基)乙基]脲
英文名称 N-[4-[(6,7-Dimethoxy-4-quinolinyl)oxy]-2-methoxyphenyl]-N'-[1-(2-thiazolyl)ethyl]urea
CAS 623142-96-1
分子式 C24H24N4O5S
分子量 480.54
MOL 文件 623142-96-1.mol
更新日期 2024/04/27 11:51:21
623142-96-1 结构式 623142-96-1 结构式

基本信息

中文别名
1-(4-((6,7-二甲基-4-基)氧基)-2-甲氧基苯基)-3-(1-(噻唑-2-基)乙基)脲
N-[4-[(6,7-二甲氧基-4-喹啉基)氧基]-2-甲氧基苯基]-N'-[1-(2-噻唑基)乙基]脲
英文别名
Ki20227
CS-1094
KI20227
KI 20227
KI20227
KI-20227
KI 20227
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
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]-
所属类别
生物化工:激动剂抑制剂

物理化学性质

沸点621.8±55.0 °C(Predicted)
密度1.327
储存条件Sealed in dry,Store in freezer, under -20°C
溶解度≥48.1 mg/mL in DMSO; insoluble in H2O; ≥8.6 mg/mL in EtOH with gentle warming and ultrasonic
酸度系数(pKa)12.03±0.46(Predicted)
形态棕色粉末。

常见问题列表

应用

 N-[4-[(6,7-二甲氧基-4-喹啉基)氧基]-2-甲氧基苯基]-N'-[1-(2-噻唑基)乙基]脲是一种 c-fms 酪氨酸激酶抑制剂,可在骨转移模型中抑制破骨细胞分化和溶骨性骨破坏。

生物活性
Ki20227 是一种口服活性的 c-Fms tyrosine kinase(CSF1R) 的高选择性抑制剂,对 c-Fms、vascular endothelial growth factor receptor-2 (KDR/VEGFR-2)、stem cell factor receptor (c-Kit) 和 platelet-derived growth factor receptor beta (PDGFRβ) 的IC50值为2 nM、12 nM、451 nM和217 nM。
靶点
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
体外研究

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.
体内研究

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.

图谱信息

Ki20227价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2024/04/30HY-10408N-[4-[(6,7-二甲氧基-4-喹啉基)氧基]-2-甲氧基苯基]-N'-[1-(2-噻唑基)乙基]脲
Ki20227
623142-96-12mg820元
2024/04/30S7688N-[4-[(6,7-二甲氧基-4-喹啉基)氧基]-2-甲氧基苯基]-N'-[1-(2-噻唑基)乙基]脲
Ki20227
623142-96-12mg1170.64元
2024/04/30HY-10408N-[4-[(6,7-二甲氧基-4-喹啉基)氧基]-2-甲氧基苯基]-N'-[1-(2-噻唑基)乙基]脲
Ki20227
623142-96-15mg1400元
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