Sapacitabine is an orally available nucleoside analog prodrug that is structurally related to cytarabine.
CAS：151823-14-2
分子式：C26H42N4O5
分子量：490.64
纯度：98%
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Background:

Sapacitabine is an orally available nucleoside analog prodrug that is structurally related to cytarabine.

Concentrations of Sapacitabine required to achieve an IC50 range from 3±0.6 uM for the colon cancer cell line HCT116 to 67±14 uM for the breast cancer cell line MDA-MB-435. Cell cycle analysis shows that 35% Sapacitabine-treated cells are arrested in late-S phase and 41% in G2/M phase. L1210 cells with deoxycytidine kinase (dCK) activity are sensitive to Sapacitabine, (IC50 20±6 uM). In the docetaxel/Sapacitabine combinations, synergistic effects (CI<1) are observed when docetaxel is given before Sapacitabine in both cell lines[1].

On Day 14, the Sapacitabine (5 mg/kg)+vorinostat (33 mg/kg) group has a mean tumour volume of 245 mm3 and a tumour growth inhibition (TGI) of 92%, whereas the Sapacitabine (15 mg/kg)+vorinostat (33 mg/kg) group has a mean tumour volume of 107 mm3 and a TGI of 112%[2].

参考文献:
[1]. Serova M, et al. Antiproliferative effects of sapacitabine (CYC682), a novel 2’-deoxycytidine-derivative, in human cancer cells. Br J Cancer. 2007 Sep 3;97(5):628-36.
[2]. Green SR, et al. Combination of sapacitabine and HDAC inhibitors stimulates cell death in AML and other tumour types. Br J Cancer. 2010 Oct 26;103(9):1391-9.