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Nutlin-3 促销  ≥98% (HPLC)

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包装规格：5mg 25mg 100mg in glass bottle
溶解性：溶于DMSO(20mg/ml)和乙醇。
产品描述：基本信息 产品编号：N10039 产品名称：Nutlin-3 CAS: 548472-68-0   储存条件 粉末 -20℃ 四年     分子式： C30H30Cl2N4O4 溶于液体 -80℃ 六个月 分子量 581.49 -20℃ 一个月 化学名：      Solubility (25°C)   体外 DMSO 100mg/mL (171.96mM) Ethanol 100mg/mL (171.96mM) 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 1.7197mL 8.5985mL 17.1969mL 5mM 0.3439mL 1.7197mL 3.4394mL 10mM 0.1720mL 0.8598mL 1.7197mL 50mM 0.0344mL 0.1720mL 0.3439mL   生物活性 产品描述 一种有效的 p53-MDM2 抑制剂，IC50：0.09μM。 靶点/IC50 Mdm2(Cell-free assay) 180nM   体外研究 Nutlin-3 is an inhibitor of the MDM2-p53 interaction. In particular, co-treatment of p53-positive HCT116 cells with 1μM of Inauhzin and 2μM of Nutlin-3 more significantly activated p53 as measured by its protein level as well as the level of its target p21, PUMA or cleaved PARP as indication of apoptosis. Nutlin-3 is a small-molecule inhibitor that acts to inhibit MDM2 binding to p53 and subsequent p53-dependent DNA damage signaling. As a single agent, Nutlin-3 (2-10μM) stabilizes p53 and p21WAF levels and is toxic to WTp53-22RV1 cells (IC50, 4.3μM) but has minimal toxicity toward p53-deficient cells (IC50, >10μM). Nutlin-3 induces p53 and p21WAF expression in a dose-dependent manner in 22RV1 cells. Short-term cell cycle assays show that, at a dose of 10μM, Nutlin-3 increasea slightly the G1-phase fraction and decreasea S-phase fraction of all three cell lines. 体内研究 Nutlin-3 can suppress the growth of xenograft tumors derived from human osteosarcoma or leukemia cells, the anti-tumor activity of Nutlin-3 even at the dose of 200mg/kg per oral administration is marginal in an HCT116-derived xenograft tumor model. Nutlin-3 may be a useful adjunct to improve the therapeutic ratio using precision radiotherapy targeted to hypoxic cells and warrants further study in vivo.   推荐实验方法(仅供参考) 激酶实验： Biacore 研究 在Biacore S51上进行竞争性实验。衍生一系列S传感器芯片CM5，用于固定 PentaHis抗体，为了捕获 His-标记的p53。捕获的水平为~200反应单位(1 反应单位对应于1 pg 蛋白/ mm2)。MDM2蛋白浓度一直维持在300nM。Nutlin-3 溶于DMSO，浓度为10mM，然后进一步稀释，在每个MDM2实验样本中产生系列浓度的Nutlin-3。在电泳缓冲液(10mM Hepes,0.15M NaCl, 2% DMSO)中25oC下进行实验。在Nutlin-3存在时，计算MDM2-p53结合情况，作为结合百分数， 使用Microsoft Excel计算IC50。   细胞实验: Human non-small-cell lung carcinoma wild type p53-containing H460 and A549, human non-small-cell lung carcinoma p53-null H1299, and human colon cancer HCT116 (p53+/+ and p53-/-) cells are used. Cells (1.5×105) are plated into 6-well plates,and incubated at 37℃ overnight. After treatment of Inauhzin and Nutlin 3 at the indicated concentrations for 48h, cells are harvested,fixed in 70% ice-cold ethanol overnight at -20℃, resuspended in propidium iodide-solution (50µg/mL PI, 0.1mg/mL RNase A, 0.05% Tritin X-100 in PBS) for 40 min at 37℃,then analyzed for DNA content using a flow cytometer and proprietary software.   动物实验: Mice Five-week-old female SCID mice are used. Mice are subcutaneously inoculated with 3×106 HCT116p53+/+ cells in the right flank and tumor growth is monitored with calipers. After the mean tumor volume reaches 50-100 mm3, animals are administered Inauhzin intraperitoneally (IP), Nutlin 3 orally, or vehicles (4% DMSO for Inauhzin, EtOH: Tween: 5% Glucose=5:5:90 for Nutlin 3). Tumor volume is measured every other day, and inhibition of tumor growth (T/C) is calculated on the last day of treatment.
保存条件：-20℃

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