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MedKoo Cat#: 563434 | Name: PQ1 Succinate
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

PQ1 Succinate is a gap junction enhancer. It acts by restoring GJIC and increasing connexin expression in breast cancer cell lines while not affecting normal mammary cells.

Chemical Structure

PQ1 Succinate
PQ1 Succinate
CAS#955995-51-4

Theoretical Analysis

MedKoo Cat#: 563434

Name: PQ1 Succinate

CAS#: 955995-51-4

Chemical Formula: C25H28F3N3O6

Exact Mass: 523.1930

Molecular Weight: 523.51

Elemental Analysis: C, 57.36; H, 5.39; F, 10.89; N, 8.03; O, 18.34

Price and Availability

Size Price Availability Quantity
5mg USD 500.00
25mg USD 1,100.00
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Related CAS #
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Synonym
PQ1 Succinate; PQ-1 Succinate; PQ 1 Succinate;
IUPAC/Chemical Name
N1-[6-Methoxy-4-methyl-5-[3-(trifluoromethyl)phenoxy]-8-quinolinyl]-1,3-propanediamine butanedioic acid salt
InChi Key
XFEIMRMBZQODRY-UHFFFAOYSA-N
InChi Code
InChI=1S/C21H22F3N3O2.C4H6O4/c1-13-7-10-27-19-16(26-9-4-8-25)12-17(28-2)20(18(13)19)29-15-6-3-5-14(11-15)21(22,23)24;5-3(6)1-2-4(7)8/h3,5-7,10-12,26H,4,8-9,25H2,1-2H3;1-2H2,(H,5,6)(H,7,8)
SMILES Code
NCCCNC1=C2N=CC=C(C)C2=C(OC3=CC=CC(C(F)(F)F)=C3)C(OC)=C1.O=C(O)CCC(O)=O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.03.00
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
PQ1 Succinate is a gap junction enhancer.
In vitro activity:
This article identified five 3-phenylquinoline derivatives as potential p53 inhibitors through screening a chemical library consisting of 120 compounds, in which PQ1 was the most active compound. PQ1 thermally stabilizes the wild-type p53 protein. Further, transcriptomics confirmed that PQ1 exposure generated a similar regulatory effect to transcription profiles with a reported p53 transcriptional inhibitor pifithrin-α. However, compared to pifithrin-α, PQ1 increased the sensitivity of SW480 cells to 5FU. Taken together, PQ1 was a novel antagonist of p53 transcriptional activity. Reference: ACS Omega. 2022 Nov 15;7(47):43180-43189. https://pubmed.ncbi.nlm.nih.gov/36467924/
In vivo activity:
The PyVT spontaneous mammary tumor mouse model was used to determine the biological and histological effects of PQ1 on tumorigenesis and metastasis at three stages of development: Pretumor, early tumor and late tumor formation. Treatment with PQ1 at all three stages of development significantly reduced tumor growth. PQ1 treatment further increased Cx43 expression during pre- and early-tumor formation, while it prevented an increase in Cx46 expression during late stage tumor formation. This study shows that Cx43 expression and neoplastic cellular growth are inversely related, but that PQ1 can alter tumor growth through targeting gap junction proteins to prove clinical efficacy in the treatment of spontaneous mammary tumors. Reference: Int J Cancer. 2014 Mar 15;134(6):1474-83. https://pubmed.ncbi.nlm.nih.gov/24038078/

Preparing Stock Solutions

The following data is based on the product molecular weight 523.51 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Wu X, Wang L, Li Z. Identification of 3-Phenylquinoline Derivative PQ1 as an Antagonist of p53 Transcriptional Activity. ACS Omega. 2022 Nov 15;7(47):43180-43189. doi: 10.1021/acsomega.2c05891. PMID: 36467924; PMCID: PMC9713874. 2. Dai Z, Zhang D, Zhang H. Design, Synthesis, and Application in OFET of a Quinoxaline-Based D-A Conjugated Polymer. Front Chem. 2022 Jun 16;10:934203. doi: 10.3389/fchem.2022.934203. PMID: 35783214; PMCID: PMC9244549. 3. Shishido SN, Delahaye A, Beck A, Nguyen TA. The anticancer effect of PQ1 in the MMTV-PyVT mouse model. Int J Cancer. 2014 Mar 15;134(6):1474-83. doi: 10.1002/ijc.28461. Epub 2013 Sep 19. PMID: 24038078; PMCID: PMC3948329. 4. Ding Y, Prasain K, Nguyen TD, Hua DH, Nguyen TA. The effect of the PQ1 anti-breast cancer agent on normal tissues. Anticancer Drugs. 2012 Oct;23(9):897-905. doi: 10.1097/CAD.0b013e328354ac71. PMID: 22569107; PMCID: PMC3428498.
In vitro protocol:
1. Wu X, Wang L, Li Z. Identification of 3-Phenylquinoline Derivative PQ1 as an Antagonist of p53 Transcriptional Activity. ACS Omega. 2022 Nov 15;7(47):43180-43189. doi: 10.1021/acsomega.2c05891. PMID: 36467924; PMCID: PMC9713874. 2. Dai Z, Zhang D, Zhang H. Design, Synthesis, and Application in OFET of a Quinoxaline-Based D-A Conjugated Polymer. Front Chem. 2022 Jun 16;10:934203. doi: 10.3389/fchem.2022.934203. PMID: 35783214; PMCID: PMC9244549.
In vivo protocol:
1. Shishido SN, Delahaye A, Beck A, Nguyen TA. The anticancer effect of PQ1 in the MMTV-PyVT mouse model. Int J Cancer. 2014 Mar 15;134(6):1474-83. doi: 10.1002/ijc.28461. Epub 2013 Sep 19. PMID: 24038078; PMCID: PMC3948329. 2. Ding Y, Prasain K, Nguyen TD, Hua DH, Nguyen TA. The effect of the PQ1 anti-breast cancer agent on normal tissues. Anticancer Drugs. 2012 Oct;23(9):897-905. doi: 10.1097/CAD.0b013e328354ac71. PMID: 22569107; PMCID: PMC3428498.
Perchellet EM, Crow KR, Gakhar G, Nguyen TA, Shi A, Hua DH, Perchellet JP. Bioactivity and molecular targets of novel substituted quinolines in murine and human tumor cell lines in vitro. Int J Oncol. 2010 Mar;36(3):673-88. doi: 10.3892/ijo_00000543. PMID: 20126988.