Acelarin

  • Chemical Properties
CAS No. 840506-29-8 Cat. No. BCP19910
Name Acelarin
Synonyms NUC-1031;NUC 1031;NUC1031;Fosgemcitabine palabenamide;CPF-31;MTL-007;GTPL7389;
Formula C25H27F2N4O8P M. Wt 580.47
  • Biological Activity
Description Acelarin is a DNA synthesis inhibitor with EC50 of 0.2 nM. Acelarin is a prodrug based on an aryloxy phosphoramidate derivative of gemcitabine. It is converted into the active metabolites dFdCDP and dFdCTP. dFdCDP can inhibit ribonucleotide reductase, thereby decreasing the deoxynucleotide pool available for DNA replication; dFdCTP can be incorporated into DNA, resulting in premature termination of DNA replication and eventually induction of apoptosis. Phase III clinical trials for the treatment of Pancreatic cancer are on-going.
Pathways Cell Cycle/DNA Damage 
Targets DNA/RNA Synthesis 

Structure

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