Gemcitabine triphosphate (dFdCTP) trisodium is the active metabolite of Gemcitabine, known for its cell-killing mechanism that involves competition with cytidine triphosphate during DNA replication, thereby inhibiting chain elongation. It partially inhibits dCMP deaminase and serves as a substrate for DNA synthesis, incorporating into cellular DNA and RNA. This leads to disruption of DNA and RNA synthesis, cell cycle arrest in G0/G1 and S phases, induction of apoptosis, and reduction of tumor cell proliferation. It is utilized in research for pancreatic cancer and non-small cell lung cancer.
- Inhibits replicative DNA polymerases α and ε
- Reduces cell viability in cancer cells
- Arrests cell cycle in S phase
- Induces caspase-3/7 activation
- Exerts antitumor effects in xenograft models
- Shows potent anti-tumor efficacy through caspase-dependent apoptosis