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STAT3-IN-1  ≥98%

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包装规格：5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性：溶于DMSO（125 mg/mL 超声）
产品描述：基本信息 产品编号： S10691 产品名称： STAT3-IN-1 CAS: 2059952-75-7   储存条件 粉末 -20℃ 四年     分子式： C28H29NO6 溶于液体 -80℃ 6个月 分子量： 475.53 -20℃ 1个月 化学名：  (E)-N-[4-[(E)-2-(3,5-dimethoxyphenyl)ethenyl]phenyl]-3-(3,4,5-trimethoxyphenyl)prop-2-enamide Solubility (25°C)：   体外:   DMSO 95mg/mL (199.77mM) Ethanol 5mg/mL (10.51mM) 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 2.1029mL 10.5146mL 21.0292mL 5mM 0.4206mL 2.1029mL 4.2058mL 10mM 0.2103mL 1.0515mL 2.1029mL 50mM 0.0421mL 0.2103mL 0.4206mL   生物活性 产品描述 是强效的、选择性的、口服有效的STAT3的抑制剂，其在HT29和MDA-MB 231 细胞中的IC50值分别为1.82μM和2.14μM。STAT3-IN-1 (compound 7d) 可诱导肿瘤细胞凋亡。 靶点 STAT3(in HT29 cells) STAT3(in MDA-MB 231 cells) 1.82μM 2.14μM   体外研究 STAT3-IN-1 (compound 7d:0-10μM,48h) inhibits the STAT3 acetylation at lysine 685 and affected its specific genes expressions.STAT3-IN-1 (compound 7d:0-10μM,48h) induces tumor cells apoptosis in MDA-MB-231 cells. Apoptosis Analysis Cell Line: MDA-MB-231 cell lines. Concentration: 0-10μM. Incubation Time: 48 hours. Result: The induced apoptosis rates (early and late apoptosis) at 1,2,5,8 and 10μM were 9.0%, 11.2%,20.9%,43.3% and 85.2% versus control 3.0%. Western Blot Analysis Cell Line: MDA-MB-231 and HT-29 cell lines. Concentration: 0-10μM. Incubation Time: 48 hours. Result: Inhibited STAT3 acetylation and STAT3 tyrosine phosphorylation in MDA-MB-231 cells.Increased the expressions of these tumor-suppressor genes (PTPN6 (SHP-1),CDKN2A and DLEC1) which were related to STAT3 acetylation at Lys685. 体内研究 STAT3-IN-1 (compound 7d:10,20mg/kg, two weeks) arrests tumor growth with low toxicity in mouse-xenograft model. Animal Model: Mouse-xenograft model bearing inoculation of mice breast cancer 4T1 cells. Dosage: 10,20mg/kg. Administration: Oral administration once every other day for two weeks. Result: Arrested tumor growth with no obvious body weight loss.
保存条件：-20℃

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