Background:

Cytarabine hydrochloride is an effective drug in the treatment of cancers of white blood cells [1].

Cytarabine hydrochloride is a dxoxycytidine (dC) analogue. Cytarabine hydrochloride has been found to be phosphorylated into a triphophate form, and thus compete with dCTP for incorporation into DNA. Cytarabine hydrochloride has reported to incorporate into DNA and block DNA synthesis by inhibiting the function of DNA and RNA polymerases. In addition, incorporated has shown a growth inhibition dose-dependent curve using acute myelogenous leukemia (AML) in a growth inhibition assay with IC50 values of 16nM,103μM and 223μM for CCRF-CEM, CEM/AraC8C and CEM/dCK-cell lines, respectively. Moreover, Cytarabine hydrochloride has been exhibited to retrovirally transducer rat leukemic KA cells by WST-1 assay with IC50 values of 0.69μM,1.73μM and 0.037μM for KA, kA/GFP and KA/wt, respectively [1,2].

参考文献:
[1] Tobias SC1, Borch RF.Synthesis and biological evaluation of a cytarabine phosphoramidate prodrug. Mol Pharm. 2004 Mar-Apr; 1(2):112-6.
[2] Veuger MJ1, Heemskerk MH, Honders MW, Willemze R, Barge RM.Functional role of alternatively spliced deoxycytidine kinase in sensitivity to cytarabine of acute myeloid leukemic cells. Blood. 2002 Feb 15; 99(4):1373-80.