| 中文名称: | IWP-2 | ||||
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| 英文名称: | IWP-2 | ||||
| 别名: | IWP-2 N-(6-Methyl-2-benzothiazolyl)-2-[(3,4,6,7-tetrahydro-4-oxo-3-phenylthieno[3,2-d]pyrimidin-2-yl)thio]-acetamide | ||||
| CAS No: | 686770-61-6 | 分子式: | C22H18N4O2S3 | 分子量: | 466.6 |
| CAS No: | 686770-61-6 | ||||
| 分子式: | C22H18N4O2S3 | ||||
| 分子量: | 466.6 | ||||
基本信息
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产品编号： |
I10286 |
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产品名称： |
IWP-2 |
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CAS: |
686770-61-6 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
两年 |
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分子量 |
466.60 |
-20℃ |
1个月 |
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化学名： |
N-(6-Methylbenzo[d]thiazol-2-yl)-2-[(4-oxo-3-phenyl-3,4,6,7-tetrahydrothieno[3,2-d]pyrimidin-2-yl)thio]acetamide |
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Solubility (25°C)： |
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体外:
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DMF |
12.5 mg/mL (26.78mM) |
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DMSO |
Insoluble |
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Water |
Insoluble |
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体内(现配现用): |
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＜1mg/ml表示微溶或不溶。 |
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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。 |
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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。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
2.1432mL |
10.7158mL |
21.4316mL |
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5mM |
0.4286mL |
2.1432mL |
4.2863mL |
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10mM |
0.2143mL |
1.0716mL |
2.1432mL |
生物活性
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产品描述 |
一种Wnt 加工和分泌的抑制剂，其 IC50 为 27nM。IWP-2 靶向膜结合的 O-酰基转移酶 porcupine (Porcn)，从而阻止关键的 Wnt 配体棕榈糖基化。 |
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靶点 |
Wnt |
M82FCK1δ |
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27nM |
40nM |
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体外研究 |
IWP-2 inhibits the proliferation of the investigated cell lines within the single digitμM range. IWP-2 inhibits cell proliferation in A818-6, MiaPaCa2, Panc-1, Panc-89, HT29, HEK293, SW620 and Capan cell with EC50s of 8.96μM, 1.90μM, 2.33μM, 3.86 μ M, 4.67μM, 2.76μM, 1.90μM and 2.05μM, respectively. Panc-1 cells are either untreated or treated with 2.33μM IWP-2 for 48 h. In IWP-2 treated cells, the CK1δ kinase peak activity is reduced to approximately 66% residual activity compared to the activity in untreated cells, respectively. IWP-2 reduces the activity of CK1δ in Panc1 cells |
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体内研究 |
To evaluate the efficacy of IWP-2 in vivo, 200 μL each of IWP-2-liposome or free liposome i separately injected into C57BL/6 mice intraperitoneally about 2 h before injection of a similar volume of either blue-dye-filled latex beads or E. coli DH5α. IWP-2 causes significant reduction in the uptake of blue beads as well as E. coli as assessed by CFUs in peritoneal lavage cells within 2 h. In addition, the levels of TNF-α and IL-6 in the lavage fluid of the corresponding mice are reduced by 2-4-fold compared with control values. Interestingly, IWP-2 even induces a considerable increase in secretion of the antiinflammatory cytokine IL-10 . |
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推荐实验方法(仅供参考)
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Cell Assay |
The human RCC cell lines 786O and Caki-2 (5×103) are seeded into 96-well plates. Cell viability is estimated by MST assay after Caki-2 acells are incubated with ncreasing concentrations of LEF together with 20μM IWP-2 for 48 h.After treatment, 10 μL MTS is added into each well for 2 h incubation. The absorbance is measured using a model ELX800 Micro Plate Reader at 490nm. For colony formation assay, Caki-2 cells are trypsinized to single cell suspensions and seeded into fresh 6-well plates at 1000 cells/well. Then cells are incubated with LEF at depicted concentrations for 7 days. Colonies are fixed with absolute methanol for 15 min and then stained with 0.1% crystal violet for 20 min. After washing with PBS three times, the colonies with a diameter over 2 mm are visualized by a digital camera |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
