中文名 | PYRVINIUM PAMOATE |
英文名 | PYRVINIUM PAMOATE |
别名 | 扑蛲灵 吡维铵 吡维氯铵 恩波吡维铵 恩波酸吡维铵 双羟萘酸扑蛲宁 USP标准品 WNT抑制剂(PYRVINIUM PAMOATE) 双[6-(二甲基氨基)-2-[2-(2,5-二甲基-1-苯基吡咯-3-基)乙烯基]-1-甲基喹啉]4,4'-亚甲基双[3-羟基-2-萘甲酸酯 |
英文别名 | molevac alnoxin pamovin altolat neo-oxypate pirviniumpamoate PYRVINIUM PAMOATE 6-(dimethylamino)-2-(2-(2,5-dimethyl-1-phenylpyrrol-3-yl)vinyl)-1-quinoliniu |
CAS | 3546-41-6 |
EINECS | 222-596-3 |
化学式 | C75H70N6O6 |
分子量 | 1151.39 |
密度 | 1.0104 (rough estimate) |
熔点 | 210-215° (softens at 190°) |
沸点 | 829.27°C (rough estimate) |
溶解度 | DMSO: >10 mg/mL |
折射率 | 1.6400 (estimate) |
存储条件 | 2-8°C |
外观 | 粉末 |
颜色 | red |
靶点 | Wnt |
体外研究 | Pyrvinium pamoate (0-500 nM) inhibits proliferation of MCF-7 (luminal), MDA-MB-231 (claudin-low), MDA-MB-468 (basal-like) and SkBr3 (HER2-OE) cells in a dose-dependent manner, with IC 50 value of 1170±105.0 nM against MDA-MB-231 cell line. Pyrvinium pamoate significantly inhibits self-renewal and proliferation of BCSCs, and suppresses BCSC population with a distinct phenotype. Pyrvinium pamoate significantly decreases average expression levels of FZD1, FZD10, WNT1, WNT7B, CTNNB1, MYC, and LRP5 at transcriptional level. Moreover, Pyrvinium pamoate also efficiently down-regulates the expression of other stemness genes including ALDH1, CD44 and ABCG2. Pyrvinium pamoate blocks colon cancer cell growth in vitro in a dose-dependent manner with great differences in the inhibitory concentration (IC 50 ), ranging from 0.6 to 65 μM for colon cancer cells with mutations in WNT signaling. Pyrvinium pamoate decreases messenger RNA (mRNA) and protein levels of known WNT target genes as c-MYC and thereby led to the induction of p21. Pyrvinium pamoate ultimately inhibits Wnt signalling despite its lack of efficacy on CK1. Pyrvinium pamoate imposes specific toxicity on cardiac fibroblasts in ischemia (IC 50 =9.5 nM). The cytotoxic effect of Pyrvinium pamoate on cardiac fibroblasts specifically under glucose- and glutamine-deficient condition. |
体内研究 | In the xenograft model, Pyrvinium pamoate (500 nM)-pretreatment strongly delays tumor size and tumor weight, and the tumor volume is markedly decreased. |
危险品标志 | Xn - 有害物品 |
风险术语 | R20/21/22 - 吸入、皮肤接触及吞食有害。 R36/37/38 - 刺激眼睛、呼吸系统和皮肤。 R40 - 少数报道有致癌后果。 |
安全术语 | S26 - 不慎与眼睛接触后,请立即用大量清水冲洗并征求医生意见。 S36 - 穿戴适当的防护服。 |
WGK Germany | 3 |
海关编号 | 2933492250 |
参考资料 展开查看 | 1. Zheng L , Liu Y , Pan J . Inhibitory effect of pyrvinium pamoate on uveal melanoma cells involves blocking of Wnt/β-catenin pathway[J].2017(49):898.2. Xu F , Zhu Y , Lu Y , et al. Anthelmintic pyrvinium pamoate blocks Wnt/β-catenin and induces apoptosis in multiple myeloma cells[J]. Oncology Letters, 2018.3. 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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 0.869 ml | 4.343 ml | 8.685 ml |
5 mM | 0.174 ml | 0.869 ml | 1.737 ml |
10 mM | 0.087 ml | 0.434 ml | 0.869 ml |
5 mM | 0.017 ml | 0.087 ml | 0.174 ml |
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