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Stauprimide  ≥98%

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包装规格：1mg 5mg in glass bottle
产品描述：基本信息 产品编号：S10730 产品名称：Stauprimide CAS: 154589-96-5   储存条件 粉末 -20℃ 四年 分子式： C35H28N4O5 溶于液体 -80℃(氮气储存) 六个月 分子量 584.62 -20℃(氮气储存) 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。   生物活性 产品描述 一种促进胚胎干细胞 (ESC) 分化的星形孢菌素类似物。Stauprimide 与 MYC 转录因子 NME2 结合并阻断其在 ESC 中的核定位，导致 MYC 转录的下调, 是一种非广谱抑制剂。 靶点/IC50 c-Myc; Autophagy 体外研究 Stauprimide (10μM; 6 hours) suppresses MYC transcription in the majority of cell lines tested with an EC50 range of 30nM-8 μM, and decreases MYC levels between 15% to over 90%.Stauprimide (2-8μM; 24-72 hours) down-regulates MYC leads to the inhibition of cell proliferation in vitro with an IC50 of 780nM in RXF 393 cells.Stauprimide (5μM; 3 hours) suppresses MYC Transcription by decreasing NME2 Nuclear Translocation.Stauprimide (4-10μM; 6 hours) acts with different EC50s and with different degrees of maximal MYC mRNA down-regulation in different cell lines. Cell Proliferation Assay Cell Line: Renal cancer cell line RXF 393 cells Concentration: 2μM, 4μM, 8μM Incubation Time: 24 hours, 48 hours, 72 hours Result: Inhibited cell proliferation at concentrations of 2-8μM. Western Blot Analysis Cell Line: Renal cancer cell line RXF 393 cells and CAKI-1 cells Concentration: 5μM Incubation Time: 3 hours Result: Decreased nuclear localized NME2. RT-PCR Cell Line: CA46 cells; Ramos cells; RXF393 cells; TK10 cells; KG1A cells; CAKI-1 cells Concentration: 4μM, 6μM, 8μM, 10μM Incubation Time: 6 hours Result: Suppressed MYC transcription in KG1A cells with an EC50 of 400±50nM and a suppression of 90%; CA46 cells were resistant to stauprimide. 体内研究 Stauprimide (oral administration; 50mg/kg; once daily; 30 days, 55 days) blocks tumor growth,reduces MYC protein levels in xenograft mouse with RXF 393 or CAKI-1 cells and inhibits MYC transcription in the RXF 393 tumor. Animal Model: Xenograft tumor models with RXF 393 and CAKI-1 cells in NOD/SCID mice Dosage: 50mg/kg Administration: Oral administration; 50mg/kg; once daily;30 days,55 days Result: Blocked tumor growth in mice injected with either RXF 393 or CAKI-1 cells during the dosing periods.
保存条件：-20℃

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