PRI-724
Catalog No.S8262
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.
Purity & Quality Control
Choose Selective Wnt/beta-catenin Inhibitors
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. | ||
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| Targets |
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| 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]. |
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| 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: |
+ Expand
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Solubility (25°C)
| In vitro | DMSO | 100 mg/mL (182.27 mM) |
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| 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 |
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| Formula | C33H32N4O4 |
| CAS No. | 847591-62-2 |
| Storage | powder |
| in solvent | |
| Synonyms | N/A |
Bio Calculators
Molarity Calculator
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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Dilution Calculator
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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
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Clinical Trial Information
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT03620474 | Recruiting | Hepatitis C|Hepatitis B|Liver Cirrhoses | Komagome Hospital|Prism Pharma Co. Ltd.|Kyushu University|National Center for Global Health and Medicine Japan|Japan Agency for Medical Research and Development | July 24 2018 | Phase 1|Phase 2 |
| NCT02413853 | Withdrawn | Colorectal Adenocarcinoma|Stage IVA Colorectal Cancer|Stage IVB Colorectal Cancer | University of Southern California|National Cancer Institute (NCI)|Prism Pharma Co. Ltd. | November 2015 | Phase 2 |
| NCT02195440 | Completed | Hepatitis C Virus-infected Cirrhosis | Komagome Hospital|Prism Pharma Co. Ltd. | August 2014 | Phase 1 |
| NCT01764477 | Completed | Advanced Pancreatic Cancer|Metastatic Pancreatic Cancer|Pancreatic Adenocarcinoma | Prism Pharma Co. Ltd.|inVentiv Health Clinical | April 2013 | Phase 1 |
| NCT01606579 | Completed | Acute Myeloid Leukemia|Chronic Myeloid Leukemia | Prism Pharma Co. Ltd.|inVentiv Health Clinical | July 2012 | Phase 1|Phase 2 |
| NCT01302405 | Terminated | Advanced Solid Tumors | Prism Pharma Co. Ltd.|inVentiv Health Clinical | February 2011 | Phase 1 |
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.
Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.
Frequently Asked Questions
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Question 1:
How to reconstitute the compound (S8262) for in vivo studies?
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Answer:
S8262 can be dissolved in 2% DMSO+30% PEG 300+5% Tween 80+ddH2O as clear solution up tp 5mg/ml.
