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TrxR inhibitor D9  

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产品描述：基本信息 产品编号：T10735 产品名称：TrxR inhibitor D9 CAS: 1527513-89-8   储存条件 粉末 -20℃ 四年 分子式： C25H20AuOPS 溶于液体 -80℃ 两年 分子量 596.43     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 一种有效和选择性的硫氧还蛋白还原酶 (TrxR) 的抑制剂，EC50 值为 2.8nM。 靶点/IC50 EC50: 2.8nM (TrxR) 体外研究 TrxR inhibitor D9 (0.1-1μM; 72h) inhibits the cell proliferation with IC50s of 0.03 and 0.1μM for MCF-7 and HT-29 cells,respectively.TrxR inhibitor D9 (72h) completely inhibits all cancer cells (A549, KB, MDA MB-231, HeLa, MCF-7 and HT-29) viability at the concentration of 0.60μM, and the IC50s of all cancer cells could be as low as 0.55μM,and dose not significantly affects normal cells viability.TrxR inhibitor D9 (0.8μM;4 and 8h) induces HT-29 cells necrosis/apoptosis.TrxR inhibitor D9 (2-20nM; 1-60 s) inhibits TrxR activity in a concentration-dependent manner.TrxR inhibitor D9 (1-1000nM) does not significantly inhibits the catalytic activity of glutathione reductase (GR) even when the concentration increases to more than 1000nM.TrxR inhibitor D9 (0.4μM) could effectively avoid the ligand exchange with albumin.Cell Proliferation Assay Cell Line: MCF-7 and HT-29 cells Concentration: 0.1, 0.5, 1μM Incubation Time: 72 hours Result: Killed 70% MCF-7 cells and 50% HT-29 cells with the concentration as low as 0.1μM. Apoptosis Analysis Cell Line: MCF-7 cells Concentration: 0.8μM Incubation Time: 4 and 8 hours Result: Led to more than 50% necrosis/apoptosis of cells compared to control after 4h of treatment.Induced all cells necrosis/apoptosis after 8h of incubation. 体内研究 TrxR inhibitor D9 (5mg/kg; i.v. once every 2 d for 15 d) effectively inhibits the growth of tumors in mice. Animal Model: BALB/c nude mice (17-18g) bearing a MCF-7 tumor Dosage: 5mg/kg Administration: I.v. once every 2 days for 15 days Result: Inhibited tumor growth with IR (inhibition ratio) of 91.5% and was well tolerated.
保存条件：-20℃

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