| 中文名称: | WHI-P180 促销 | ||||
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| 英文名称: | WHI-P180 | ||||
| 别名: | 3-[(6,7-dimethoxyquinazolin-4-yl)amino]phenol | ||||
| CAS No: | 211555-08-7 | 分子式: | C16H15N3O3 | 分子量: | 297.31 |
| CAS No: | 211555-08-7 | ||||
| 分子式: | C16H15N3O3 | ||||
| 分子量: | 297.31 | ||||
基本信息
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产品编号：W10002 |
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产品名称：WHI-P180 |
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CAS: |
211555-08-7 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
两年 |
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分子量 |
297.31 |
-20℃ |
一个月 |
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化学名： |
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Solubility (25°C) |
体外 |
DMSO |
59mg/mL (198.44mM) |
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Ethanol |
Insoluble |
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Water |
Insoluble |
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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。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
3.3635mL |
16.8175mL |
33.6349mL |
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5mM |
0.6727mL |
3.3635mL |
6.7270mL |
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10mM |
0.3363mL |
1.6817mL |
3.3635mL |
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50mM |
0.0673mL |
0.3363mL |
0.6727mL |
生物活性
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产品描述 |
一种有效的EGFR和CDK2抑制剂，IC50分别为4μM和1μM。 |
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靶点/IC50 |
RET |
KDR |
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4.5nM |
66nM |
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体内研究 |
WHI-P180 is also an active inhibitor of IgE-mediated mast cell responses. The elimination half-life of WHI-P180 in CD-1 mice(BALB/c mice) following i.v., i.p., or p.o. administration is less than 10min. Systemic clearance of WHI-P180 is 6742mL/h/kg in CD-I mice and 8188mL/h/kg in BALB/c mice. Notably, WHI-P180, when administered in two consecutive nontoxic i.p.bolus doses of 25mg/kg, inhibits IgE/antigen-induced vascular hyperpermeability in a well-characterized murine model of passive cutaneous anaphylaxis. |
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推荐实验方法(仅供参考)
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激酶实验： |
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Kinase Assay |
Inhibitors (WHI-P180) are pre-incubated in the plate for 15 min with 5μL kinase and assay buffer at the following concentrations; 13pM RET and 150pM KDR. The reaction is initiated by the addition of 5μL ATP and substrate at 2×final reaction concentrations. For RET, this is 18μM and 2μM; for KDR, this is 16μM and 1μM, respectively. Reactions are performed at ATP Km for each target. The assay is allowed to proceed at room temperature for 20 min before terminating with the addition of 10μL HTRF detection buffer containing EDTA supplemented with TK-antibody labelled with Eu3+- Cryptate (1:100 dilution) and streptavidin-XL665 (128nM). Following incubation at room temperature for 1 h, FRET signal is measured. |
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细胞实验: |
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Cell Assay |
IL3-dependent BaF3 cells are modified to express an activated recombinant kinase. Following removal of IL3, the modified cells are dependent on the activity of the recombinant kinase for survival and proliferation. The BaF3 cell lines, expressing KIF5B-RET and KDR are maintained in RPMI-1640 media containing 10% FBS and appropriate antibiotics. Non-modified BaF3 cells (WT) are maintained in RPMI-1640 media containing 10% FBS and supplemented with 10ng/mL recombinant mouse IL3. For assessment of compound IC50, cells are plated into 384-well plates at 1500 or 3000 cells per well in 30μL culture medium and compounds dispensed using an acoustic liquid handling platform. Following incubation of the cells for 48h at 37 °C in a humidified 5% CO2 atmosphere, viability is determined by addition of 10μL CellTiter-Glo reagent and measurement of luminescence. |
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动物实验: |
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Animal Administration |
Mice: A high performance liquid chromatography (HPLC)-based quantitative detection method is used to measure plasma WHI-P180levels in mice. The plasma concentration-time data is fit to a single compartment pharmacokinetic model by using the WinNonlin program to calculate the pharmacokinetic parameters. A cutaneous anaphylaxis model is used to examine the pharmacodynamic effects of WHI-P180 on anaphylaxis-associated vascular hyperpermeability. |
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 )
