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RC-3095, a Gastrin-Releasing Peptide Receptor Antagonist, Synergizes With Gemcitabine to Inhibit the Growth of Human Pancreatic Cancer CFPAC-1 in Vitro and in Vivo

RC-3095, a Gastrin-Releasing Peptide Receptor Antagonist, Synergizes With Gemcitabine to Inhibit the Growth of Human Pancreatic Cancer CFPAC-1 in Vitro and in Vivo

Shu-Kun Hong, Shi-Yong Yang, Shao-Hua Yin, Kun-Xing Yang

Pancreas. 2014 Jan;43(1):15-21.

PMID: 24326363

Abstract:

Objectives:
Pancreatic cancer remains a lethal disease. In this study, we investigated the efficacy of a combination of gastrin-releasing peptide receptor antagonist RC-3095 and gemcitabine on pancreatic cancer CFPAC-1.
Methods:
The antiproliferation effects of RC-3095, gemcitabine, or the combination on pancreatic cancer were monitored in vitro. Nude mice bearing xenografts of CFPAC-1 cell received injections of the vehicle (control), RC-3095 (20 μg, subcutaneously, daily), gemcitabine (15 mg/kg, intraperitoneally, every 3 days), or the combination of RC-3095 and gemcitabine for 4 weeks. The histological changes and protein expression were tested using immunohistochemistry and Western blotting.
Results:
Treatment with the combination in culture exhibited a powerful inhibition effect on CFPAC-1 cell proliferation. In xenograft mice model, RC-3095 or gemcitabine significantly reduced the volume and weight of tumors after 4 weeks of treatment, as compared with controls. The combination more potently inhibited the tumor growth than either agent used individually. Immunohistochemistry and Western blotting showed gastrin-releasing peptide receptor/bombesin receptor subtype-3 positive cells and protein expression in tumors decreased by treatment with RC-3095 or gemcitabine alone or greater in combination.
Conclusions:
Our data suggested that the combination could be considered for the possible new approaches for treatment of pancreatic cancers.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP138147781	RC-3095		138147-78-1	Price

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