Pyrvinium pamoate is an FDA-approved antihelmintic drug that inhibitsWNTpathway signaling.

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 IC₅₀value 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^[1]. Pyrvinium pamoate blocks colon cancer cell growth in vitro in a dose-dependent manner with great differences in the inhibitory concentration (IC₅₀), 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^[2]. Pyrvinium pamoate ultimately inhibits Wnt signalling despite its lack of efficacy on CK1^[3]. Pyrvinium pamoate imposes specific toxicity on cardiac fibroblasts in ischemia (IC₅₀=9.5 nM). The cytotoxic effect of Pyrvinium pamoate on cardiac fibroblasts specifically under glucose- and glutamine-deficient condition^[4].

In the xenograft model, Pyrvinium pamoate (500 nM)-pretreatment strongly delays tumor size and tumor weight, and the tumor volume is markedly decreased^[1].

575.70

Solid

C₂₆H₂₈N₃.1/2 C₂₃H₁₄O₆

3546-41-6

扑蛲灵；吡维铵；吡维氯铵；恩波酸吡维铵；恩波吡维铵

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DMSO : 17.86 mg/mL(31.02 mM;Need ultrasonic)

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