Discovery of a Novel Potent and Orally Efficacious PGK1 Inhibitor C67–47 for the Treatment of Human Pancreatic Cancer
) of 63 nM and exhibits potent antiproliferative effects in pancreatic cancer cells. In preclinical studies, C67-47 demonstrated excellent oral pharmacokinetics in both mouse and rat models. Strikingly, a single oral dose of C67-47 resulted in up to 80% tumor growth inhibition in pancreatic cancer xenograft models with no observable toxicity. These findings establish C67-47 as a promising lead compound for the development of orally administered, PGK1-targeted therapies for pancreatic cancer.
Authors
- Xin Han (ORCID: https://orcid.org/0000-0002-9620-7502)
- Hongli Yang (ORCID: https://orcid.org/0009-0006-0106-6011)
- S B Li
- Shudi Luo (ORCID: https://orcid.org/0000-0002-3696-2469)
- 聂豆
- Lihua Liu (ORCID: https://orcid.org/0000-0001-5078-0656)
- Xiaoming Jiang (ORCID: https://orcid.org/0000-0002-1363-7292)
- Zou Lu
- Lihui Wu (ORCID: https://orcid.org/0000-0003-1977-8122)
- Qingqing Yang (ORCID: https://orcid.org/0000-0001-6214-3750)
- Dong Guo
- Hao Yang
- Hong Zhao
Institutions
- Center for Translational Molecular Medicine (NL)
- Ministry of Education (ET)
- First Affiliated Hospital Zhejiang University (CN)
- Zhejiang University (CN)
Publication Details
- Journal
- Journal of Medicinal Chemistry
- Published
- 2026-05-29
- DOI
- https://doi.org/10.1021/acs.jmedchem.5c03549
- Primary Topic
- Metabolism, Diabetes, and Cancer
- Type
- article
- Field-Weighted Citation Impact
- 0.00
Funders
- National Natural Science Foundation of China
- Ministry of Science and Technology of the People's Republic of China