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WHI-P180 hydrochloride  ≥98%

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包装规格：5mg 10mg in glass bottle
产品描述：基本信息 产品编号：W10049 产品名称：WHI-P180 hydrochloride CAS: 153437-55-9   储存条件 粉末 -20℃ 四年 分子式： C16H16ClN3O3 分子量 333.77 化学名：  3-((6,7-Dimethoxyquinazolin-4-yl)amino)phenol hydrochloride   生物活性 产品描述 一种多种激酶抑制剂；抑制RET，KDR和EGFR的IC50值分别为5nM，66nM和4μM。 靶点/IC50 EGFR 4μM(IC50) KDR 66nM(IC50) RET 5nM(IC50)   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 8188 mL/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.   推荐实验方法(仅供参考) 激酶实验： Inhibitors (WHI-P180) are pre-incubated in the plate for 15 min with 5μL kinase and assay buffer at the following concentrations; 13 pM RET and 150 pM 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 20min 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 1h, FRET signal is measured.   细胞实验:   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 10 μL CellTiter-Glo reagent and measurement of luminescence.   动物实验:   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. 给药处理 i.p.
保存条件：-20℃

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