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PD 158780  ≥98%(HPLC)

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包装规格：5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性：溶于DMSO(21mg/mL)。
产品描述：基本信息 产品编号：P10117 产品名称：PD 158780 CAS: 171179-06-9   储存条件 粉末 -20℃ 四年     分子式： C14H12BrN5 溶于液体 -80℃ 六个月 分子量 330.19 -20℃ 一个月 化学名：      Solubility (25°C)   体外 DMSO   Ethanol   Water   体内（现配现用）     ＜1mg/ml表示微溶或不溶。 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。 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 3.0287mL 15.1433mL 30.2865mL 5mM 0.6057mL 3.0287mL 6.0573mL 10mM 0.3029mL 1.5143mL 3.0287mL   生物活性 产品描述 一种EGFR(表皮生长因子受体)抑制剂。 靶点/IC50 EGFR 8μM (IC50, Cell Assay) ErbB2 49nM (IC50, Cell Assay) ErbB3 52nM (IC50, Cell Assay) ErbB4 52nM (IC50, Cell Assay)   体外研究 PD158780 inhibits EGF receptor autophosphorylation in A431 human epidermoid carcinoma with IC50 value of 13 nM.PD158780 is highly specific for the EGF receptor in Swiss 3T3 fibroblasts, inhibiting EGF-dependent receptor autophosphorylation and thymidine incorporation at low nanomolar concentrations while requiring micromolar levels for platelet-derived growth factor- and basic fibroblast growth factordependent processes. PD158780 inhibits heregulinstimulated phosphorylation in the SK-BR-3 and MDAMB-453 breast carcinomas with IC50 values of 49 and 52nM,respectively,suggesting that the compound is active against other members of the EGF receptor family.   体内研究 PD158780 is active against clone formation in several breast tumors having different expression patterns of the ErbB family.PD158780 shows good therapeutic effect against the A431 epidermoid carcinoma when administered either intraperitoneally or orally. PD158780 produces measurable, significant effects against a mouse fibroblast transfected with human EGFR. PD158780 produces a significant therapeutic effect against the estrogendependent MCF-7 breast carcinoma at equitoxic dose levels.   推荐实验方法(仅供参考) 激酶实验： The enzyme assay is performed in 96-well filter plates. The total volume is 0.1 mL containing 20 mM HEPES, pH 7.4, 50μM sodium vanadate, 40mM magnesium chloride, 10μM ATP containing 0.5μCi of [32p]ATP, 20μg of polyglutamic acid/tyrosine, 1ng of EGF receptor tyrosine kinase, ard appropriate dilutions of inhibitor (PD158780) and/or ATP. All corrtponents except the ATP are added to the well, and the plate is incubated with shaking for 10min at 25°C. The reaction is started by adding [32p]ATP, and the plate is incubated with shaking at 25°C for 10 min. The reaction is terminated by the addition of 0.1mL of 20% TCA, and the plate is kept at 4°C for at least 15min to allow the substrate to precipitate. The wells are then ished five times with 0.125mL of 10% TCA, and [32p] incorporation is determined.   细胞实验:   All cell lines are maintained as monolayers in dMEM/F12, 50:50 containing 10% fetal bovine serum. For growth inhibition assays, dilutions of the designated compound (PD158780) in 10μL are placed in 24-well plates followed by the addition of cells in 2mL of medium. The plates are incubated for 72hr at 37°C in a humidified atmosphere. Cell growth is determined by counting cells.   动物实验:   Tumor fragments were implanted sc into the right axilla of mice on day 0. PD158780 is administered intraperitoneally or orally. Tumor growth is monitored.
保存条件：-20℃

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