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扑蛲灵
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CAS号:3546-41-6 | 英文名称:Pyrvinium pamoate
分子式
分子量
EINECS号
MDL
Smiles
InChIKey
乙二醇化学百科
基本信息
中文名称 Pyrvinium pamoate salt hydrate
英文名称 Pyrvinium pamoate salt hydrate
CAS号 3546-41-6
分子式 C75H72N6O7
分子量 1169.41018
EINECS号 222-596-3
物化性质
熔点 210-215° (softens at 190°)
沸点 829.27°C (rough estimate)
密度 1.0104 (rough estimate)
折射率 1.6400 (estimate)
溶解度 二甲基亚砜:>10mg/mL
形态 粉末
颜色 红色
安全信息
危险品标志 Xn
危险类别码 20/21/22-36/37/38-40
安全说明 26-36
WGK Germany 3
海关编码 2933492250
生产及用途
Pyrvinium是一种驱虫剂,对蛲虫有效。

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.

In the xenograft model, Pyrvinium pamoate (500 nM)-pretreatment strongly delays tumor size and tumor weight, and the tumor volume is markedly decreased.

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