中文名称: Napabucasin
英文名称: Napabucasin
CAS No: 83280-65-3
分子式: C14H8O4
分子量: 240.21
N10189 Napabucasin ≥98% (psaitong)
包装规格:
25mg 100mg in glass bottle
溶解性:
溶于DMSO
产品描述:

基本信息

产品编号:

N10189

产品名称:

Napabucasin

CAS:

83280-65-3

 

储存条件

粉末

-20℃

四年

 

 

分子式:

C14H8O4

溶于液体

-80℃

6个月

分子量:

240.21

-20℃

1个月

化学名: 

2-Acetyl-4H,9H-naphtho[2,3-b]furan-4,9-dione

Solubility (25°C):

 

体外:

 

DMSO

14mg/mL (58.28mM)

Ethanol

Insoluble

Water

Insoluble

体内(现配现用):

5% DMSO+40% PEG 300+5% Tween 80+ddH2O

1mg/mL

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

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:

 

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:

 

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.

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
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