中文名称: | Tyrosine kinase-IN-1 | ||||
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英文名称: | Tyrosine kinase-IN-1 | ||||
别名: | Tyrosine kinase-IN-1 (3Z)-5-[(1-ethylpiperidin-4-yl)amino]-3-[(3-fluorophenyl)-(5-methyl-1H-imidazol-2-yl)methylidene]-1H-indol-2-one | ||||
CAS No: | 705946-27-6 | 分子式: | C26H28FN5O | 分子量: | 445.5424 |
CAS No: | 705946-27-6 | ||||
分子式: | C26H28FN5O | ||||
分子量: | 445.5424 |
基本信息
产品编号:T11337 |
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产品名称:Tyrosine kinase-IN-1 |
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CAS: |
705946-27-6 |
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 |
445.54 |
-20℃ |
一个月 |
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化学名: |
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Solubility (25°C) |
体外 |
DMSO |
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Ethanol |
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Water |
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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 |
2.2445mL |
11.2226mL |
22.4452mL |
5mM |
0.4489mL |
2.2445mL |
4.4890mL |
10mM |
0.2245mL |
1.1223mL |
2.2445 mL |
生物活性
产品描述 |
一种多靶点的酪氨酸激酶抑制剂,抑制 KDR,Flt-1,FGFR1 和 PDGFRα 的 IC50 值分别为4,20,4,2nM。 |
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靶点/IC50 |
Flt-1 4nM (IC50) |
KDR 20nM (IC50 |
PDGFRα 4nM (IC50) |
FGFR1 2nM (IC50) |
体外研究 |
Tyrosine kinase-IN-1 is from reference (compound 8K) |
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体内研究 |
Tyrosine kinase-IN-1 shows a reasonable PK profile (AUC(0–∞)=1.9, t1/2=4.6h). It has a favorable oral bioavailability (F=63%) in rats. |
推荐实验方法(仅供参考)
激酶实验: |
Kinase Inhibition Assays Kinase activities of KDR and PDGFRα are measured as the percent of ATP consumed following the kinase reaction using luciferaseluciferin-coupled chemiluminescence.Kinase reactions are initiated by combining test compound (Tyrosine kinase-IN-1), ATP, kinases and substrates in a 20mL volume using 384-well microtiter plates. For KDR,the final reaction mixture contained 3mM ATP, 1.6 mM poly(Glu, Tyr) 4:1 and 1.5nM KDR of residues D807-V1356 with an Nterminal GST tag. For PDGFRα, the final reaction mixture contained 2mM ATP, 10mM MBP and 14 nM PDGFRα of residues Q551-L1089 with an N-terminal GST tag. The reaction mixture is incubated at room temperature for 4 h (KDR) or 2h PDGFRα before a 20mL aliquot of Kinase Glo is added and luminescence signal is measured using a Victor2 plate reader.Total ATP consumption is limited below 50%. |
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 )