CA-5f  ≥98%

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包装规格:5mg 10mg 25mg 50mg in glass bottle
溶解性:溶于DMSO(77.5 mg/mL 超声)
产品描述:基本信息 产品编号:C10821  产品名称:CA-5f CAS: 1370032-19-1   储存条件 粉末 -20℃ 四年     分子式: C24H24N2O3 溶于液体 -80℃ 两年 分子量 388.46 -20℃ 一个月 化学名:  (E)-3-((1H-Indol-3-yl)methylene)-5-((E)-3,4-dimethoxybenzylidene)-1-methylpiperidin-4-one   Solubility (25°C)   体外 DMSO 78mg/mL (200.79mM) Ethanol Insoluble 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 2.5743mL 12.8713mL 25.7427mL 5mM 0.5149mL 2.5743mL 5.1485mL 10mM 0.2574mL 1.2871mL 2.5743mL 50mM 0.0515mL 0.2574mL 0.5149mL   生物活性 产品描述 一种有效的晚期巨自噬/自噬 (macroautophagy/autophagy) 抑制剂,通过抑制自噬体-溶酶体融合起作用。 靶点/IC50 Macroautophagy/autophagy   体外研究 CA-5f (0-40μM, 6 hour) concentration- and time-dependently elevates the level of LC3B-II (a marker to monitor autophagy)and SQSTM1 protein both in A549 cells and HUVECs. CA-5f (20μM, 6 hours) inhibits the degradation of autophagosomes when treated alone or in combination Bafilomycin A1(100nM) or Chloroquine (30μM) in A549 cells and HUVECs. CA-5f (20μM) neither impairs the hydrolytic function nor the quantity of lysosomes. CA-5f (20μM, 96 hours) inhibits the growth of A549 cells, and less cytotoxic to normal HUVECs. Cell Viability Assay Cell Line: A549, HUVECs Concentration: 20μM Incubation Time: 96 hours Result: Exhibited more cytotoxicity against A549 cells compared with normal HUVECs. Western Blot Analysis Cell Line: A549 cells and HUVECs Concentration: 0-40μM Incubation Time: 6 hours Result: Elevated LC3B-II (a marker to monitor autophagy) and SQSTM1 protein levels in a concentration- and time-dependent manner.   体内研究 CA-5f (40 mg/kg, i.p., every 2 days for up to 30 days) is well tolerated, and potently inhibits the growth of tumor in nude mice bearing A549 lung cancer cells. CA-5f (40 mg/kg, i.p.) suppresses autophagic flux and induces apoptosis in nude mice bearing A549 lung cancer cells. Animal Model: Nude mice bearing A549 lung cancer cells Dosage: 40 mg/kg Administration: Injected via caudal vein, every 2 days for up to 30 days Result: Significantly suppressed tumor volume and weight in mice, increased the number of apoptotic cells in mice.
保存条件:-20℃