Pyrvinium pamoate

Modify Date: 2024-01-11 11:08:36

Pyrvinium pamoate Structure
Pyrvinium pamoate structure
Common Name Pyrvinium pamoate
CAS Number 3546-41-6 Molecular Weight 575.70
Density 1.0104 (rough estimate) Boiling Point 829.27°C (rough estimate)
Molecular Formula C26H28N3.1/2C23H14O6 Melting Point 210-215° (softens at 190°)
MSDS N/A Flash Point N/A
Symbol GHS07 GHS08
GHS07, GHS08
Signal Word Warning

 Use of Pyrvinium pamoate


Pyrvinium pamoate is an FDA-approved antihelmintic drug that inhibits WNT pathway signaling.

 Names

Name Pyrvinium pamoate
Synonym More Synonyms

 Pyrvinium pamoate Biological Activity

Description Pyrvinium pamoate is an FDA-approved antihelmintic drug that inhibits WNT pathway signaling.
Related Catalog
In Vitro 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 IC50 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[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 Vivo In the xenograft model, Pyrvinium pamoate (500 nM)-pretreatment strongly delays tumor size and tumor weight, and the tumor volume is markedly decreased[1].
Cell Assay 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 Admin 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.

 Chemical & Physical Properties

Density 1.0104 (rough estimate)
Boiling Point 829.27°C (rough estimate)
Melting Point 210-215° (softens at 190°)
Molecular Formula C26H28N3.1/2C23H14O6
Molecular Weight 575.70
PSA 144.82000
LogP 12.33840
Appearance of Characters red
Index of Refraction 1.6400 (estimate)
Storage condition room temp
Water Solubility DMSO: >10mg/mL

 Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
VC3543500
CAS REGISTRY NUMBER :
3546-41-6
LAST UPDATED :
199512
DATA ITEMS CITED :
11
MOLECULAR FORMULA :
C75-H70-N6-O6
MOLECULAR WEIGHT :
1151.51
WISWESSER LINE NOTATION :
T66 BKJ B1 HN1&1 C1U1- CT5NJ AR& B1 E1 &L66J CQ DVO B1- BL66J CQ DVO

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
5 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
200 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Behavioral - tremor
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
15 gm/kg/30D-C
TOXIC EFFECTS :
Endocrine - other changes Related to Chronic Data - death Related to Chronic Data - changes in testicular weight

MUTATION DATA

TYPE OF TEST :
Gene conversion and mitotic recombination
TEST SYSTEM :
Yeast - Saccharomyces cerevisiae
DOSE/DURATION :
400 umol/L
REFERENCE :
MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 187,79,1987 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - 81965 No. of Facilities: 805 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 805 (estimated) NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - 81965 No. of Facilities: 19 (estimated) No. of Industries: 1 No. of Occupations: 2 No. of Employees: 774 (estimated) No. of Female Employees: 337 (estimated)

 Safety Information

Symbol GHS07 GHS08
GHS07, GHS08
Signal Word Warning
Hazard Statements H302 + H312 + H332-H315-H319-H335-H351
Precautionary Statements P261-P280-P301 + P312 + P330-P305 + P351 + P338
Hazard Codes Xn
Risk Phrases 20/21/22-36/37/38-40
Safety Phrases 26-36
RIDADR NONH for all modes of transport

 Articles1

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 Synonyms

pyrvinium pamoate
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