Ki20227
- CAS号:623142-96-1
- 英文名:N-[4-[(6,7-Dimethoxy-4-quinolinyl)oxy]-2-methoxyphenyl]-N'-[1-(2-thiazolyl)ethyl]urea
- 中文名:Ki20227
- CBNumber:CB42484677
- 分子式:C24H24N4O5S
- 分子量:480.54
- MOL File:623142-96-1.mol
- 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
- 形态 :Brown powder.
- 酸度系数(pKa) :12.03±0.46(Predicted)
- 颜色 :Off-white to pink
Ki20227性质、用途与生产工艺
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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。
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靶点
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 -
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.
- 更新日期：2024/11/08
- 产品编号：HY-10408
- 产品名称：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 Ki20227
- CAS编号：623142-96-1
- 包装：2mg
- 价格：700元
- 更新日期：2024/11/08
- 产品编号：HY-10408
- 产品名称：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 Ki20227
- CAS编号：623142-96-1
- 包装：5mg
- 价格：1200元
- 公司名称：ACTIVATE
- 联系电话：--
- 电子邮件：info@activate-scientific.com
- 国家：德国
- 产品数：2856
- 优势度：61
