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SC144 hydrochloride  ≥98%

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包装规格：5mg in glass bottle
溶解性：溶于DMSO（10 mg/mL 超声）
产品描述：基本信息 产品编号： S10702 产品名称： SC144 hydrochloride CAS: 917497-70-2   储存条件 粉末 -20℃ 四年     分子式： C16H12ClFN6O 溶于液体 -80℃ 6个月 分子量： 358.76 -20℃ 1个月 化学名：  2-(7-Fluoropyrrolo[1,2-a]quinoxalin-4-yl)hydrazide-2-pyrazinecarboxylic acid hydrochloride 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。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.7874mL 13.9369mL 27.8738mL 5mM 0.5575mL 2.7874mL 5.5748mL 10mM 0.2787mL 1.3937mL 2.7874mL   生物活性 产品描述 是首创的口服活性gp130 (IL6-beta)抑制剂。SC144 hydrochloride结合gp130，诱导gp130磷酸化(S782)和去糖基化，消除Stat3磷酸化和核易位，进一步抑制下游靶基因的表达。 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: I.p;daily for 58 days Administration: 10mg/kg Result: Significantly inhibited tumor growth by about 73%.
保存条件：-20℃

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