中文名称: | 1-(4-((6,7-Dimethoxyquinolin-4-yl)oxy)-2-methoxyphenyl)-3-(1-(thiazol-2-yl)ethyl)urea | ||||
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英文名称: | 1-(4-((6,7-Dimethoxyquinolin-4-yl)oxy)-2-methoxyphenyl)-3-(1-(thiazol-2-yl)ethyl)urea | ||||
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 Ki20227 | ||||
CAS No: | 623142-96-1 | 分子式: | C24H24N4O5S | 分子量: | 480.539 |
CAS No: | 623142-96-1 | ||||
分子式: | C24H24N4O5S | ||||
分子量: | 480.539 |
基本信息
产品编号:K10157 |
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产品名称:1-(4-((6,7-Dimethoxyquinolin-4-yl)oxy)-2-methoxyphenyl)-3-(1-(thiazol-2-yl)ethyl)urea |
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CAS: |
623142-96-1 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式: |
溶于液体 |
-80℃ |
六个月 |
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分子量 |
480.54 |
-20℃ |
一个月 |
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化学名: |
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Solubility (25°C) |
体外 |
DMSO |
96mg/mL (199.77mM) |
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Ethanol |
3mg/mL (6.24mM) |
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Water |
˂1mg/mL |
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体内(现配现用) |
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<1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
2.0810mL |
10.4050mL |
20.8099mL |
5mM |
0.4162mL |
2.0810mL |
4.1620mL |
10mM |
0.2081mL |
1.0405mL |
2.0810mL |
50mM |
0.0416mL |
0.2081mL |
0.4162mL |
生物活性
产品描述 |
一种口服有效,高选择性 CSF1R (c-Fms 酪氨酸激酶)抑制剂,对 CSF1R,VEGFR2 (血管内皮生长因子受体 2),c-Kit (干细胞因子受体) 和 PDGFRβ (血小板衍生的生长因子受体 β) 的 IC50 分别为 2 nM,12 nM,451 nM 和 217 nM。Ki20227 可以抑制破骨细胞分化和溶骨性破坏。 |
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靶点/IC50 |
c-Fms(Cell-free assay) |
VEGFR2 |
PDGFRβ |
c-Kit |
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2nM |
12nM |
217nM |
451nM |
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体外研究 |
Ki20227 (0.1-1000nM; 72 hours) with 100 and 1,000nM almost suppresses M-NFS-60 cell growth and HUVEC cell growth,respectively.Ki20227 (0.1-1000nM; 1 hour) suppresses M-CSF-dependent c-Fms phosphorylation in a dose-dependent manner. Cell Viability Assay |
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Cell Line: |
M-NFS-60 cells, HUVEC cells, human A375 melanoma cells |
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Concentration: |
0.1, 0.3, 1, 3, 10, 30, 100, 300, 1000 nM |
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Incubation Time: |
72 hours |
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Result: |
100 and 1,000 nM almost suppressed M-NFS-60 cell growth and HUVEC cell growth, respectively. |
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Cell Viability Assay |
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Cell Line: |
RAW264.7 cell lysate |
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Concentration: |
0.1, 0.3, 1, 3, 10, 30, 100, 300, 1000 nM |
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Incubation Time: |
1 hour |
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Result: |
Suppressed M-CSF-dependent c-Fms phosphorylation in a dose-dependent manner. |
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体内研究 |
Ki20227 (orally;10-50mg/kg/d for 20 days) of 50mg/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. |
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Animal Model: |
4-week-old male F344/NJcl-rnu rats |
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Dosage: |
10, 20, and 50 mg/kg |
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Administration: |
Orally; once per day for 20 days |
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Result: |
Oral administration of 50 mg/kg/d markedly decreased the osteolytic lesion areas. |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )