Ki20227

应用生物活性靶点体外研究体内研究 Ki20227 试剂级价格

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

Ki20227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
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

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
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.