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PD153035 Hydrochloride  ≥98%

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包装规格：25mg 100mg 250mg in glass bottle
溶解性：溶于DMSO（5mg/ml）
产品描述：基本信息 产品编号：P11583 产品名称：PD153035 Hydrochloride CAS: 183322-45-4   储存条件 粉末 -20℃ 四年 分子式： C16H14BrN3O2.HCl 溶于液体 -80℃ 两年 分子量 396.67     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 2.5210mL 12.6049mL 25.2099mL 5mM 0.5042mL 2.5210mL 5.0420mL 10mM 0.2521mL 1.2605mL 2.5210mL   生物活性 产品描述 一种有效的EGFR抑制剂，Ki和IC50值分别为6和25pM。 靶点/IC50 EGFR 6pM (Ki) EGFR 25pM (IC50)   体外研究 PD153035 inhibits EGF-stimulated receptor autophosphorylation in A431 human epidermoid carcinoma cells, with an IC50 of 14nM. PD153035 has little effect on PDGFR, FGFR, CSF-1 receptor, the insulin receptor, or on src tyrosine kinases at concentrations as high as 50μM. PD153035 rapidly suppresses autophosphorylation of the EGF receptor at low nanomolar concentrations in fibroblasts or in human epidermoid carcinoma cells and selectively blocks EGF-mediated cellular processes including mitogenesis, early gene expression, and oncogenic transformation. PD153035 causes a dosedependent growth inhibition of EGF receptor-positive cell lines, beginning at less than micromolar concentrations, and theIC50 is less than 1pM in most cases.   体内研究 PD153035 levels in the plasma and tumor rise to 50 and 22μM within 15 minutes following a single i.p. dose of 80 mg/kg. While the plasma levels of PD 153035 falls below 1μM by 3 hours, in the tumors it remains at micromolar concentrations for at least 12 hours. The tyrosine phosphorylation of the EGF receptor is rapidly suppressed by 80-90% in the tumors.   推荐实验方法(仅供参考) 细胞实验:   Different EGF receptor-overexpressing cell lines (A43 1, Difi, MDA-MB-468, MDA-MB-231, DU145, SiHa, C4i, and MEl 80) are treated with PD153035 at increasing concentrations of 0.125-2.5p.M. Growth inhibitory effect in monolayer cell culture is assessed.   动物实验:   Mice: Mice are injected with PD153035 (80mg/kg) or vehicle and rumors are excised at 20 minutes and 180 minutes and extracts are prepared. Two mice are used for each time point and the experiment is repeated four times. Within each of the four experiments ANOVA is used to compare the inhibition by PD 153035 of the EGF-stimulation.
保存条件：-20℃

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