PRI-724

Catalog No.S8262

PRI-724 Chemical Structure

Molecular Weight(MW): 548.63

PRI-724 is a potent, specific inhibitor of the canonical Wnt signaling pathway in cancer stem cells with potential antineoplastic activity. PRI-724 specifically inhibits the recruiting of beta-catenin with its coactivator CBP.

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  • Real-time PCR for FAS

    Biochim Biophys Acta, 2018, doi: 10.1016/j.bbalip.2018.04.008. PRI-724 purchased from Selleck.

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Biological Activity

Description PRI-724 is a potent, specific inhibitor of the canonical Wnt signaling pathway in cancer stem cells with potential antineoplastic activity. PRI-724 specifically inhibits the recruiting of beta-catenin with its coactivator CBP.
Targets
Wnt/β-catenin [1]
150 nM
In vitro

PRI-724 binds specifically to CBP but not the related transcriptional coactivator p300, thereby disrupting the interaction of CBP with β-catenin. Treatment with PRI-724 selectively induces apoptosis in colon carcinoma cells but not in normal colonic epithelial cells and reduces in vitro growth of colon carcinoma cells[1][2].

In vivo PRI-724 exhibits antitumor activity in the mouse xenograft models of colon cancer. The initial results of the Phase I clinic trial of PRI-724 has been disclosed publically. The drug exhibits an acceptable toxicity profile with only one dose-limiting toxicity of grade 3 reversible hyperbilirubinaemia. An Open-Label dose-escalation phase I/II study of PRI-724 for patients with advanced myeloid malignancies is still ongoing[2].

Protocol

Animal Research:

[3]

+ Expand
  • Animal Models: C57BL/6 and Balb/c mice
  • Formulation: PBS
  • Dosages: 0.4 mg/mouse
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (182.27 mM)
Ethanol 100 mg/mL (182.27 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 548.63
Formula

C33H32N4O4

CAS No. 847591-62-2
Storage powder
in solvent
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

  • Question 1:

    How to reconstitute the compound (S8262) for in vivo studies?

  • Answer:

    S8262 can be dissolved in 2% DMSO+30% PEG 300+5% Tween 80+ddH2O as clear solution up tp 5mg/ml.

Wnt/beta-catenin Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID