Pyrvinium pamoate (Pyrvinium embonate)
(Synonyms: 扑蛲灵,Pyrvinium embonate) 目录号 : GC32698
An anthelmintic and anticancer agent
Cas No.:3546-41-6
Sample solution is provided at 25 µL, 10mM.
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)
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. | |
| Cas No. | 3546-41-6 | SDF | |
| 别名 | 扑蛲灵,Pyrvinium embonate | ||
| Canonical 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 |
| 溶解度 | DMSO : ≥ 24 mg/mL (41.69 mM) | 储存条件 | 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℃，然后在超声波浴中震荡一段时间。 |
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| 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。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.737 mL | 8.6851 mL | 17.3702 mL |
| 5 mM | 0.3474 mL | 1.737 mL | 3.474 mL |
| 10 mM | 0.1737 mL | 0.8685 mL | 1.737 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet