Dalpiciclib

  • Chemical Properties
CAS No. 1637781-04-4 Cat. No. BCP45155
Name Dalpiciclib
Synonyms SHR-6390; SHR6390; SHR 6390;
Formula C25H30N6O2 M. Wt 446.54
  • Biological Activity
Description Dalpiciclib, also known as SHR-6390, is a cyclin-dependent kinase (CDK) inhibitor with potential antineoplastic activity. SHR6390 exhibited potent antiproliferative activity against a wide range of human RB‐positive tumor cells in vitro, and exclusively induced G1 arrest as well as cellular senescence, with a concomitant reduction in the levels of Ser780‐phosphorylated RB protein. Compared with the well‐known CDK4/6 inhibitor palbociclib, orally administered SHR6390 led to equivalent or improved tumor efficacy against a panel of carcinoma xenografts, and produced marked tumor regression in some models, in association with sustained target inhibition in tumor tissues. Furthermore, SHR6390 overcame resistance to endocrine therapy and HER2‐targeting antibody in ER‐positive and HER2‐positive breast cancer, respectively. Moreover, SHR6390 combined with endocrine therapy exerted remarkable synergistic antitumor activity in ER‐positive breast cancer.
Pathways Cell Cycle/DNA Damage 
Targets CDK 

Structure

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