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Pelitinib  ≥98%（HPLC）

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外观与性状：白色至类白色固体
包装规格：5mg 25mg 100mg in glass bottle
溶解性：溶于DMSO(5mg/mL 加热）
产品描述：基本信息 产品编号：P10102 产品名称：Pelitinib CAS: 257933-82-7   储存条件 粉末 -20℃ 四年     分子式： C24H23ClFN5O2 溶于液体 -80℃ 六个月 分子量 467.92 -20℃ 一个月 化学名：      Solubility (25°C)   体外 DMSO 13mg/mL (27.78mM) Ethanol Insoluble Water Insoluble 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 2.1371mL 10.6856mL 21.3712mL 5mM 0.4274mL 2.1371mL 4.2742mL 10mM 0.2137mL 1.0686mL 2.1371mL   生物活性 产品描述 一种EGFR(表皮生长因子受体)抑制剂，IC50:38.5nM。 靶点/IC50 EGFR 38.5nM (IC50)   体外研究 Pelitini has much greater inhibitory activity against the EGFR kinase than against Src, MEK/ERK, Cdk4, c-Met, Raf and ErbB2,for example, the IC50 for EGFR is 32-fold lower than the IC50 for the closely related ErbB2. Pelitinib results in a dramatic reduction in EGFR phosphorylation but no change in the total amount of EGFR protein. It requires at least 10-fold more drug to equivalently inhibit ErbB2 phosphorylation in similar assays, and EKB-569 does not block phosphorylation of another receptor tyrosine kinase (c-Met) assessed in the same manner[1]. EKB-569 is a potent inhibitor of proliferation in NHEK, A431,and MDA-468 cells (IC50=61, 125, and 260nM, respectively) but not MCF-7 cells (IC50=3600nM). EKB-569 is also a potent inhibitor of EGF-induced phosphorylated EGF-R (pEGF-R) in A431 and NHEK cells (IC50=20-80nM).   体内研究 A single oral dose of 10mg/kg EKB-569 inhibits EGFR phosphorylation in A431 xenografts within 60minutes. Twenty-four hours later, EGFR activity is still inhibited by over 50% by this single oral dose. The half-life of EKB-569 in mouse plasma is about 2hours.   推荐实验方法(仅供参考) 细胞实验:   For experiments using cells in culture, A431 cells or 3T3/c-erbB-2 cells over-expressing c-erbB2 are are treated with various concentrations of EKB-569 for 2.75 h before co-incubation with 100ng/mL EGF (A431 cells) or no growth factor (3T3/c-erbB2 cells) for 0.25h. Cells are ished twice with cold phosphate-buffered saline (PBS) before adding to lysis buffer for 20min on ice, before immunoprecipitation and SDS–PAGE-immunoblotting.   动物实验:   Mice: For in vivo experiments, athymic nu/nu female mice are implanted subcutaneously with 5×106 A431 tumor cells. When tumors reach a mass of 200-300mg, animals are treated with a single dose of 10mg/kg EKB-569 in pH 2.0 water per gavage.Tumors from control and drug-treated animals are excised and minced into 1-mm pieces for anlysis.
保存条件：-20℃

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