SC144  ≥98%

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包装规格:5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性:溶于DMSO(16.67 mg/mL 超声)
产品描述:基本信息 产品编号: S10688 产品名称: SC144 CAS: 895158-95-9   储存条件 粉末 -20℃ 四年     分子式: C16H11FN6O 溶于液体 -80℃ 6个月 分子量: 322.30 -20℃ 1个月 化学名:  N'-(7-fluoropyrrolo[1,2-a]quinoxalin-4-yl)-2-pyrazinecarbohydrazi De Solubility (25°C):   体外:   DMSO 64mg/mL (198.57mM) Ethanol Insoluble Water Insoluble 体内(现配现用): 30% propylene glycol,5% Tween 80,65% D5W 30mg/mL <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 3.1027mL 15.5135mL 31.0270mL 5mM 0.6205mL 3.1027mL 6.2054mL 10mM 0.3103mL 1.5513mL 3.1027mL 50mM 0.0621mL 0.3103mL 0.6205mL   生物活性 产品描述 是首创的口服活性gp130 (IL6-beta)抑制剂。 靶点 IL6-beta   体外研究 SC144 inhibits cell growth in a panel of human ovarian cancer cell lines with IC50s in a submicromolar range (IC50=OVCAR-8,OVCAR-5,OVCAR-3=0.72,0.49,0.95μM).The potency of SC144 toward NCI/ADR-RES (Paclitaxel-and Doxorubicin-resistant,IC50=0.43μM) and HEY (Cisplatinresistant,IC50=0.88μM) suggests an ability to overcome drug resistance in ovarian cancer.SC144 (2μM;24 hours) causes significantly more apoptosis in OVCAR-8 and Caov-3 than normal kidney epithelial and normal endometrial cells.SC144 (0.5-2μM;0-6 hours) substantially increases the phosphorylation of gp130 (S782) in both OVCAR-8 and Caov-3 cells in a time-and dose-dependent manner.SC144 is cytotoxic to ovarian cancer cells via a mechanism involving the inhibition of gp130 activity,leading to the inactivation of Akt and Stat3 as well as the suppression of Stat3-regulated gene expression.As are result,SC144 treatment eventually causes cell-cycle arrest,anti-angiogenesis,and apoptosis. Apoptosis Analysis Cell Line: OVCAR-8 and Caov-3 cells Concentration: 2μM Incubation Time: 24 hours Result: Significantly caused cell death in OVCAR-8 and Caov-3 cells. Western Blot Analysis Cell Line: OVCAR-8,Caov-3 cells Concentration: 0.5-2μM Incubation Time: 0-6 hours Result: Substantially increased the phosphorylation of gp130 (S782) in both OVCAR-8 and Caov-3 cellsin a time- and dose-dependent manner. 体内研究 SC144 (10mg/kg;i.p.;daily for 58 days) suppresses tumor growth in human ovariancancer xenografts.SC144 (100mg/kg;p.o.;daily for 35 days) treatment shows the average tumor volume in mice 82% smaller than that in the control group. Animal Model: Athymic mice (human ovarian cancer xenograft) Dosage: 10mg/kg Administration: I.p;daily for 58 days Result: Significantly inhibited tumor growth by about 73%.   推荐实验方法(仅供参考) 细胞实验:   细胞系 OVCAR-8,OVCAR-5,OVCAR-3,Caov-3,SKOV-3,HEY NCI/ADR-RES 浓度 ~10μM 处理时间 96小时 方法 MTT检测   动物实验:   动物模型 人卵巢癌OVCAR-8异种移植 剂量 10毫克/千克,每天 给药处理 腹腔注射或口服
保存条件:-20℃