2. Academic Validation
  3. Discovery of ZN-c3, a Highly Potent and Selective Wee1 Inhibitor Undergoing Evaluation in Clinical Trials for the Treatment of Cancer

Discovery of ZN-c3, a Highly Potent and Selective Wee1 Inhibitor Undergoing Evaluation in Clinical Trials for the Treatment of Cancer

  • J Med Chem. 2021 Sep 9;64(17):13004-13024. doi: 10.1021/acs.jmedchem.1c01121.
Peter Q Huang 1,  Brant C Boren 1,  Sayee G Hegde 1,  Hui Liu 1,  Aditya K Unni 1,  Sunny Abraham 1,  Chad D Hopkins 1,  Sunil Paliwal 1,  Ahmed A Samatar 1,  Jiali Li 1,  Kevin D Bunker 1
Affiliations

Affiliation

  • 1 Zentalis Pharmaceuticals, San Diego, California 92121, United States.
PMID: 34423975 DOI: 10.1021/acs.jmedchem.1c01121
Abstract

Wee1 inhibition has received great attention in the past decade as a promising therapy for Cancer treatment. Therefore, a potent and selective Wee1 Inhibitor is highly desirable. Our efforts to make safer and more efficacious Wee1 inhibitors led to the discovery of compound 16, a highly selective Wee1 Inhibitor with balanced potency, ADME, and pharmacokinetic properties. The chiral ethyl moiety of compound 16 provided an unexpected improvement of Wee1 potency. Compound 16, known as ZN-c3, showed excellent in vivo efficacy and is currently being evaluated in phase 2 clinical trials.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-132295
    99.84%, Wee1 Inhibitor