Cytarabine-13C3 is intended for use as an internal standard for the quantification of cytarabine by GC- or LC-MS. Cytarabine is a nucleoside analog that differs from cytosine by the presence of a hydroxyl group at the 2' position of the sugar residue. It is triphosphorylated in vivo to produce ara-C, a competitive inhibitor of DNA polymerases α and β (Kis = 4 and 32 μM, respectively).1,2,3 At low concentrations, ara-C is incorporated into DNA, slowing but not stopping DNA synthesis.4 It has antiviral activity against certain types of viruses.5 Formulations containing cytarabine have been used in the treatment of leukemia.4
|1. Furth, J.J., and Cohen, S.S. Inhibition of mammalian DNA polymerase by the 5'-triphosphate of 1-β-D-arabinofuranosylcytosine and the 5'-triphosphate of 9-β-D-arabinofuranoxyladenine. Cancer Res. 28(10), 2061-2067 (1968).|2. Graham, F.L., and Whitmore, G.F. Studies in mouse L-cells on the incorporation of 1-β-D-arabinofuranosylcytosine into DNA and on inhibition of DNA polymerase by 1-β-D-arabinofuranosylcytosine 5'-triphosphate. Cancer Res. 30(11), 2636-2644 (1970).|3. Yoshida, S., Yamada, M., and Masaki, S. Inhibition of DNA polymerase-α and -β of calf thymus by 1-β-D-arabinofuranosylcytosine-5'-triphosphate. Biochim. Biophys. Acta. 477(2), 144-150 (1977).|4. Pourquier, P., Takebayashi, Y., Urasaki, Y., et al. Induction of topoisomerase I cleavage complexes by 1-β-D-arabinofuranosylcytosine (ara-C) in vitro and in ara-C-treated cells. Proc. Nat. Acad. Sci. USA 97(4), 1885-1890 (2000).|5. Volmer, R., Bajramovic, J.J., Schneider, U., et al. Mechanism of the antiviral action of 1-β-D-arabinofuranosylcytosine on Borna disease virus. J. Virol. 79(7), 4514-4518 (2005).