中文名称: | Napabucasin | ||||
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英文名称: | Napabucasin | ||||
别名: | BBI608(Napabucasin)那布卡辛;2-乙酰基呋喃-1,4-萘醌;2-乙酰基呋喃并-1,4-萘醌;i>]呋喃-4,9-二酮 2-Acetylfuro-1,4-naphthoquinone | ||||
CAS No: | 83280-65-3 | 分子式: | C14H8O4 | 分子量: | 240.21 |
CAS No: | 83280-65-3 | ||||
分子式: | C14H8O4 | ||||
分子量: | 240.21 |
基本信息
产品编号: |
N10189 |
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产品名称: |
Napabucasin |
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CAS: |
83280-65-3 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式: |
溶于液体 |
-80℃ |
6个月 |
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分子量: |
240.21 |
-20℃ |
1个月 |
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化学名: |
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Solubility (25°C): |
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体外:
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DMSO |
14mg/mL (58.28mM) |
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Ethanol |
Insoluble |
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Water |
Insoluble |
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体内(现配现用): |
5% DMSO+40% PEG 300+5% Tween 80+ddH2O |
1mg/mL |
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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。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
4.1630mL |
20.8151mL |
41.6302mL |
5mM |
0.8326mL |
4.1630mL |
8.3260mL |
10mM |
0.4163mL |
2.0815mL |
4.1630mL |
50mM |
0.0833mL |
0.4163mL |
0.8326mL |
生物活性
产品描述 |
一种STAT3的抑制剂。 |
靶点 |
STAT3 |
体外研究 |
Napabucasin inhibits the expressions of stemness markers and kill stemness-high cancer cells isolated from several kinds of tumors except PCa.Napabucasin not only inhibits cell proliferation,cell motility,cell survival,colony formation ability,and tumorigenic potential of PCa cells,and increases cell apoptosis and sensitivity to docetaxel,but also effectively blocks sphere formation of PrCSCs and kill them as well as inhibits stemness gene expression.Napabucasin inhibits cell proliferation in PC-3 cells and 22RV1 cells at 48,72,96,and 120h (P<0.05).Cell motility and colony formation ability are closely correlated with the process of tumor metastasis.Napabucasin significantly decreases colony formation and cell motility ability of PCa cell lines in vitro (P<0.05).The proliferation of PC-3 and 22RV1 cells treated with 1μM Napabucasin are significantly decreased from day 2 to 5 compared with the control group (P<0.05). |
体内研究 |
Napabucasin (40mg/kg) or Docetaxel significantly reduces xenograft tumor growth and tumor volume (TV) compared with PBS (P<0.05).Notably,while no differences are observed between the Napabucasin and the docetaxel groups in PC-3 mouse xenograft models,the TV in Napabucasin group is even lower than docetaxel group in 22RV1 mouse xenograft models (P<0.05).Additionally,Napabucasin or docetaxel also significantly reduces tumor weight compared with PBS (P<0.05). |
推荐实验方法(仅供参考)
细胞实验: |
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The antiproliferative activity of Napabucasin against the PCa cell lines PC-3 and 22RV1 is examined.For cell proliferation assay,the PCa cell lines (22RV1 and PC-3) are seeded in 96-well plates at 2×103 cells/well in a final volume of 100μL and incubated overnight.The proliferation of PC-3 and 22RV1 cells treated with 1μM Napabucasin.The viability of cells is determined with CellTiter 96 non-radioactive cell proliferation assay (MTS).For colony formation assay,cells are placed in a six-well plate and maintained in RPMI-1640 supplemented with 10% FBS for 2 weeks.The colonies are fixed with 4% paraformaldehyde,stained with 0.1% crystal violet and counted. |
动物实验: |
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Mice A total of 1×106 PC-3 cells or 8×106 22RV1 cells in 100μL of PBS are injected subcutaneously into dorsal flanks of an immunodeficient nude mouse.The animals are treated i.p.with Napabucasin (40mg/kg),Docetaxel (10mg/kg),or PBS q3d once the tumors have reached 50 mm3.The tumor volume (TV) is calculated every 4 days according to the following standard formula:TV (mm3)=length×width2×0.5. |
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 )