MT 63-78  

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产品描述:基本信息 产品编号:M10799 产品名称:MT 63-78 CAS: 1179347-65-9   储存条件 粉末 -20℃ 四年 分子式: C21H14N2O2 溶于液体 -80℃(避光) 六个月 分子量: 326.35 -20℃(避光) 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。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 3.0642mL 15.3210mL 30.6419mL 5mM 0.6128mL 3.0642mL 6.1284mL 10mM 0.3064mL 1.5321mL 3.0642mL   生物活性 产品描述 一种有效的直接 AMPK 激活剂,EC50 为 25μM。M 63-78 还诱导细胞有丝分裂阻滞和细胞凋亡 (apoptosis)。 靶点/IC50 AMPK 25μM (EC50) mTORC1   体外研究 MT 63-78 (0-50μM;4 days;LNCaP and PC3 cells) treatment shows a dose-dependent decrease in cell number,and concomitant to the activation of AMPK signaling.MT 63-78 (25μM;24 hours;LNCaP and CRPC cells) treatment induces a significant enrichement in the G2/M population.MT 63-78 (0-50μM;24 hours;LNCaP,PC3,C4-4,C4-2B,CL1and 22RV1cells) treatment induces reduction of anti-apoptotic Mcl-1 in concert with accumulation of the pro-apoptotic BH3-only protein Puma.MT 63-78 (0-50μM;30 minutes;LNCaP and PC3 cells) treatment shows a dose-dependent phosphorylation of the two major AMPK targets Acetyl-CoA Carboxylase (ACC) on Ser79 and of Raptor on Ser792.And also increases Thr172 phosphorylation on the AMPK α subunit. Cell Viability Assay Cell Line: LNCaP and PC3 cells Concentration: 0μM,1μM,5μM,10μM,25μM,50μM Incubation Time: 4 days Result: A dose-dependent decrease in cell numberconcomitant to the activation of AMPK signaling was observed. Cell Cycle Analysis Cell Line: LNCaP and CRPC cells Concentration: 25μM Incubation Time: 24 hours Result: Induced a significant enrichement in the G2/M population in both androgen sensitive and CRPC cell models. Apoptosis Analysis Cell Line: LNCaP, PC3, C4-4, C4-2B, CL1and 22RV1cells Concentration: 0μM,10μM,25μM,50μM Incubation Time: 24 hours Result: Induced reduction of anti-apoptotic Mcl-1 in concert with accumulation of the proapoptotic BH3-only protein Puma in all PCa cells. Western Blot Analysis Cell Line: LNCaP and PC3 cells Concentration: 0μM,0.25μM,0.5μM,1μM,5μM,25μM,50μM Incubation Time: 30 minutes Result: Observed a dose-dependent phosphorylation of the two major AMPK targets Acetyl-CoA Carboxylase (ACC) on Ser79 and of Raptor on Ser792.A corresponding increase in Thr172 phosphorylation on the AMPK α subunit was also observed. 体内研究 MT 63-78 (30mg/kg;intraperitoneal injection;daily;for 14 days;C57 BL/6 male mice) treatment leads to a 33% inhibition of tumor growth. Animal Model: C57 BL/6 male mice bearing LNCaP tumors Dosage: 30mg/kg Administration: Intraperitoneal injection;daily;for 14 days Result: Led to a 33% inhibition of tumor growth.
保存条件:-20℃