MilliporeSigma™ Calbiochem™ Gemcitabine, HCl

Description

• A bioavailable, moderately toxic, deoxyctytidine analog with anti-metabolite and anti-tumor properties
• Shown to be effective against a variety of tumors and blocks the growth of cancer cells in culture (IC 50 = 8.7, 57, 3.7, and 36nM for L1210, CEM, Caco2, and HeLa cells, respectively)
• Following its uptake into cells by nucleoside transporters it is phosphorylated to its mono (dFdCMP), di (dFdCDP), and triphosphorylated (dFdCTP) forms by deoxycytidine kinase
• dFdCDP and dFdCTP are reported to inhibit the activity of ribonucleotide reductase and impede DNA synthesis and repair mechanisms and induce cell death
• Blocks the progression of cells through the G1/S phase
• The dFdCTP is shown to compete with endogenous deoxycytidine triphosphate (dCTP) for incorporation into DNA and against CTP into RNA
• Gemcitabine is also shown to block mitochondrial DNA polymerase γ
• Works synergistically with other chemotherapeutic agents to enhance their cytotoxicity
• Its half life is reported to be 42 to 94 min (depending upon the age and sex of the individual).