Product Type: Inhibitor
CAS No.: 122111-03-9
MolecularFormula: C9H11F2N3O4 • HCl
Molecular Weight: 299,7
Source: Synthetic
Purity: >98% (HPLC); NMR (Conforms)
Solubility: May be dissolved in DMSO (20 mg/ml); or Water (25 mg/ml)
Appearance: Off-white powder
PubChem CID: 60749
Scientific Background: A clinically useful anticancer agent.1 It exerts its cytotoxic effects via the metabolites gemcitabine diphosphate (dFdCDP) and gemcitabine triphosphate (dFdCTP). dFdCTP is an inhibitor of DNA polymerase and is incorporated into DNA resulting in termination of chain elongation and apoptosis. dFdCDP is an inhibitor of ribonucleotide reductase which results in depletion of deoxyribonucleotides needed for DNA synthesis. The phosphates have also been reported to inhibit cytidine triphosphate synthetase (CTP synthetase)2 and deoxycytidylate deaminase (dCMP deaminase)3. Topoisomerase 1 has also been shown to be a target for gemcitabine.4
References: 1. Mini E., et al. (2006) Ann. Oncol. 17 Suppl 5:v7.2. Heinemann V., et al. (1995) Semin. Oncol. 22(4 Suppl 11):11.3. Heinemann V., et al. (1992) Cancer Res. 52:533.4. Pourquier P., et al. (2002) Clin. Cancer Res. 8:2499.
Field of Use: Not for use in humans. Not for use in diagnostics or therapeutics. For in vitro research use only.