PRI-724

Synonyms: C-82 prodrug, ICG-001 analog

PRI-724 (C-82 prodrug, ICG-001 analog) is a potent and specific inhibitor that disrupts the interaction of β-catenin and CBP.

PRI-724 Chemical Structure

PRI-724 Chemical Structure

CAS: 1422253-38-0

Selleck's PRI-724 has been cited by 27 publications

Purity & Quality Control

Batch: Purity: 99.12%
99.12

Products often used together with PRI-724

Vismodegib (GDC-0449)


PRI-724 and Vismodegib synergistically inhibit the migration of head and neck squamous cancer cells.

Kleszcz R, et al. Int J Mol Sci. 2023 Jun 21;24(13):10448.

Erlotinib


PRI-724 and Erlotinib induce apoptosis in head and neck squamous cancer cells.

Kleszcz R, et al. Int J Mol Sci. 2023 Jun 21;24(13):10448.

HS-173


PRI-724 and HS-173 synergistically reduce the viability of FaDu cells.

Kleszcz R, et al. Int J Mol Sci. 2023 Jun 21;24(13):10448.

LGK-974


PRI-724 and LGK-974 exhibit antitumor properties in NET cell lines.

Jin XF, et al. Cancers (Basel). 2020 Feb 4;12(2):345.

ICG-001


PRI-724 and ICG-001 are antifibrotic compounds that inhibit Wnt signaling and prevent liver fibrosis.

Duspara K, et al. J Clin Transl Hepatol. 2021 Dec 28; 9(6): 960–971.

PRI-724 Related Products

Choose Selective Wnt/beta-catenin Inhibitors

Biological Activity

Description PRI-724 (C-82 prodrug, ICG-001 analog) is a potent and specific inhibitor that disrupts the interaction of β-catenin and CBP.
Targets
β-catenin [1] CBP [1]
In Vivo
In vivo

PRI-724 reduces liver fibrosis,and hepatic hydroxyproline levels, in HCV mice while attenuating αSMA induction. PRI-724 leads to increased levels of matrix metalloproteinase (MMP)-8 mRNA in the liver, along with elevated levels of intrahepatic neutrophils and macrophages/monocytes. In conclusion, PRI-724 ameliorates HCV-induced liver fibrosis in mice. PRI-724 is a drug candidate which possesses antifibrotic effect.[1]

Animal Research Animal Models HCV GT1b transgenic mice (MxCre+/−/CN2-29+/−)
Dosages 5 mg/kg, 15 mg/kg, 20 mg/kg; 1 mg/kg
Administration IP/SC
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04688034 Completed
Liver Cirrhosis
Kiminori Kimura MD|Japan Agency for Medical Research and Development|Ohara Pharmaceutical Co. Ltd.|Komagome Hospital
March 15 2021 Phase 1
NCT04047160 Completed
Primary Biliary Cholangitis (PBC)|Liver Cirrhosis Biliary
Kiminori Kimura MD|Ohara Pharmaceutical Co. Ltd.|Japan Agency for Medical Research and Development|Komagome Hospital
August 29 2019 Phase 1
NCT02195440 Completed
Hepatitis C Virus-infected Cirrhosis
Komagome Hospital|Prism Pharma Co. Ltd.|Japan Agency for Medical Research and Development
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

Chemical Information & Solubility

Molecular Weight 658.64 Formula
C33H35N6O7P
CAS No. 1422253-38-0 SDF --
Smiles CC1C2N(C(C(=O)N1CC3=CC=CC4=C3N=CC=C4)CC5=CC=C(C=C5)OP(=O)(O)O)C(=O)CN(N2C(=O)NCC6=CC=CC=C6)C
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (151.82 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

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In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

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