Pyrvinium pamoate (Pyrvinium embonate)

目录号: GC32698纯度: >98.00%同义词: 扑蛲灵,Pyrvinium embonate
An anthelmintic and anticancer agent

Pyrvinium pamoate (Pyrvinium embonate)
Cas No.: 3546-41-6
规格价格库存数量操作
10mg¥491.00现货
1
50mg¥884.00现货
1
100mg¥1,384.00现货
1
10mM (in 1mL DMSO)¥540.00现货
1

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产品描述 Description

Pyrvinium is an anthelmintic and anticancer agent.1,2 Dietary administration of pyrvinium reduces worm burden in mouse models of N. dubius, S. obvelata, or A. tetraptera infection (EC50s = 292, 4, and 17 ppm, respectively) but is lethal to mice at higher concentrations (LC50 = 600 ppm).1 Pyrvinium (1 μg/ml) induces cytotoxicity in PANC-1 cells cultured in glucose-deficient medium but not serum- or amino acid-deficient medium or complete medium.2 It reduces tumor growth in a PANC-1 mouse xenograft model when administered at a dose of 100 μg/mouse per day. Pyrvinium (10 nM) also binds to and activates casein kinase 1α (CK1α).3 It inhibits Wnt signaling (EC50 = ~10 nM in a reporter assay) in a CK1α-dependent manner. Formulations containing pyrvinium were previously used in the treatment of pinworm infections.

1.Brody, G.L., and Elward, T.E.Comparative activity of 29 known anthelmintics under standardized drug-diet and gavage medication regimens against four helminth species in miceJ. Parasitol.57(5)1068-1077(1971) 2.Esumi, H., Lu, J., Kurashima, Y., et al.Antitumor activity of pyrvinium pamoate, 6-(dimethylamino)-2-[2-(2,5-dimethyl-1-phenyl-1H-pyrrol-3-yl)ethenyl]-1-methyl-quinolinium pamoate salt, showing preferential cytotoxicity during glucose starvationCancer Sci.95(8)685-690(2004) 3.Van Acker, H.H., Capsomidis, A., Smits, E.L., et al.CD56 in the immune system: More than a marker for cytotoxicity?Front. Immunol.8892(2017)

实验参考方法 Experimental Reference Method

Cell experiment:

Pyrvinium pamoate is dissolved in DMSO at a concentration of 1 μM and is stocked in aliquots at -20°C. Cells (1×104) are suspended in 200 μL culture medium and then seeded into 96-well plates in quintuplicate overnight. Cells are treated with indicated concentrations of Pyrvinium pamoate (0-8,000 μM). After incubating for 3 days, CCK8 (10 μL) is added into each well and incubated at 37°C for 1 h. The absorbance is measured using a microplate reader at 450 nm[1].

Animal experiment:

Mice: NOD/SCID mice are housed under aseptic conditions in individually ventilated cages. For xenografting, 5×106 Pyrvinium pamoate-pretreated or untreated breast cancer cells (MDA-MB-231) are resuspended in a 1:1 mixture of culture medium and Matrigel and then transplanted into the fourth pair of mammary fat pads of mice (4-6-week-old). After injection, tumor size is measured by calipers each day and tumor growth is plotted. Upon reaching the endpoint, mice are sacrificed and tumors are harvested. All the tumors are formalin-fixed, and paraffin-embedded for hematoxylin and eosin and immunohistochemical staining[1].

References:

[1]. Xu L, et al. WNT pathway inhibitor pyrvinium pamoate inhibits the self-renewal and metastasis of breast cancer stem cells. Int J Oncol. 2016 Mar;48(3):1175-86.
[2]. Wiegering A, et al. The impact of pyrvinium pamoate on colon cancer cell viability. Int J Colorectal Dis. 2014 Oct;29(10):1189-98.
[3]. Venerando A, et al. Pyrvinium pamoate does not activate protein kinase CK1, but promotes Akt/PKB down-regulation and GSK3 activation. Biochem J. 2013 May 15;452(1):131-7.
[4]. Murakoshi M, et al. An anthelmintic drug, pyrvinium pamoate, thwarts fibrosis and ameliorates myocardial contractile dysfunction in a mouse model of myocardial infarction. PLoS One. 2013 Nov 4;8(11):e79374.

产品文档 Product Documents

Purity:>98.00%

化学性质Chemical Properties

CAS 号
3546-41-6
同义词
扑蛲灵,Pyrvinium embonate
SMILES
C[N+]1=C2C=CC(N(C)C)=CC2=CC=C1/C=C/C3=C(C)N(C4=CC=CC=C4)C(C)=C3.C[N+]5=C6C=CC(N(C)C)=CC6=CC=C5/C=C/C7=C(C)N(C8=CC=CC=C8)C(C)=C7.O=C(C9=C(O)C(CC%10=C%11C=CC=CC%11=CC(C([O-])=O)=C%10O)=C%12C=CC=CC%12=C9)[O-]
分子式
C26H28N3 . 1/2 C23H14O6
分子量
575.7 g/mol
溶解性
DMSO : ≥ 24 mg/mL (41.69 mM)
保存条件
4°C, protect from light ,unstable in solution, ready to use.
General tips
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。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至 37°C,然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备 RT,或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol