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June 1, 2026Journal of Medicinal Chemistry0 citations

Discovery of a Novel Potent and Orally Efficacious PGK1 Inhibitor C67–47 for the Treatment of Human Pancreatic Cancer

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LLLihua LiuXJXiaoming JiangHZHong Zhao

Key Points

  • To evaluate the efficacy and pharmacokinetics of C67-47 as a PGK1 inhibitor for pancreatic cancer treatment.
  • Investigated the antiproliferative effects of C67-47 on pancreatic cancer cells
  • Assessed oral pharmacokinetics in mouse and rat models
  • Evaluated tumor growth inhibition using pancreatic cancer xenograft models.
  • C67-47 exhibited a potency of 63 nM in inhibiting cancer cell proliferation
  • Achieved up to 80% inhibition of tumor growth in xenograft models
  • No observable toxicity was recorded with a single oral dose.

Abstract

) 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.

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Cite This Study

Liu et al. (2026) studied this question.

synapsesocial.com/papers/6a1d21ba02fbce9130637ac6https://doi.org/10.1021/acs.jmedchem.5c03549
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