JW55  ≥98%(HPLC)

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包装规格:5mg 25mg 100mg in glass bottle
溶解性:溶于DMSO(≥50mg/mL)
产品描述:基本信息 产品编号:J10023 产品名称:JW55 CAS: 664993-53-7   储存条件 粉末 -20℃ 四年     分子式: C25H26N2O5 溶于液体 -80℃ 两年 分子量 434.48 -20℃ 一个月 化学名:  N-(4-(((4-(4-methoxyphenyl)tetrahydro-2H-pyran-4-yl)methyl)carbamoyl)phenyl)furan-2-carboxamide   Solubility (25°C)   体外 DMSO 87mg/mL (200.23mM) Ethanol 4mg/mL (9.2mM) 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 2.3015mL 11.5077mL 23.0155mL 5mM 0.4603mL 2.3015mL 4.6031mL 10mM 0.2302mL 1.1508mL 2.3015mL 50mM 0.0460mL 0.2302mL 0.4603mL   生物活性 产品描述 一种有效的选择性β-catenin抑制剂,通过抑制端锚聚合酶(TNKS1/2)发挥作用。 靶点/IC50 TNKS2 0.83μM (IC50) TNKS1 1.9μM (IC50)   体外研究 JW 55 (JW55) is a potent and selective inhibitor of the canonical Wnt pathway. Wnt3a-induced HEK293 cells containing a transiently transfected ST-Luc (SuperTop-luciferase) reporter show inhibition by JW55 with an IC50 value of 470 nM. JW55 is effective in the range of 1 to 5μM in SW480 cells and 0.01 to 5μM in HCT-15 cells. JW55 is effective in the range of 1 to 5μM in SW480 cells and 0.01 to 5μM in HCT-15 cells.   体内研究 JW 55 (100mg/kg, orally) reduces tumor development in conditional Apc knockout mice. JW55 reduces XWnt8-induced axis duplication inXenopus embryos and Tamoxifen-induced polyposis formation in conditional APC mutant mice.   推荐实验方法(仅供参考) 细胞实验: Cell Assay A total of 1,000 SW480 or RKO cells are seeded in 96-well plates. The day after, the cell culture medium is exchanged to solutions that contained 0.1% DMSO or 10μM JW55 for RKO cells and 0.1% DMSO or 10, 5, or 1μM JW55 for SW480 cells. All samples consist of a minimum of 6 replicates. The plate is incubated in an IncuCyte inside a cell culture incubator. Images are captured every second hour to monitor proliferation.   动物实验:   Animal Administration Mice Seven 12-week old female ApcCKO/CKO/Lgr5-CreERT2 mice are injected intraperitonally with 25mg/kg of Tamoxifen diluted in an ethanol and corn oil (ratio 1:4). The mice are randomized into 2 groups and treated with either JW55 (100 mg/kg) or vehicle (DMSO). Daily per oral applications started the day after and continued for 3 weeks. The mouse body weight is measured twice a week. The mice are sacrificed and the intestines are dissected, washed in PBS, and fixed in formaldehyde [10% solution (v/v) in PBS]. The small intestines are stained using 1% methylene blue prepared in 10% paraformalaldehyde (PFA)/PBS solution. Small ileum Swiss-rolls are embedded in paraffin sectioned and stained with hematoxylin and eosin. Fixed colons are embedded in paraffin, sectioned and stained with an anti-β-catenin antibody. The number and size of the intestinal lesions are quantified by the Ellipse program.
保存条件:-20℃