N-[1-[(2R,3S,4S,5R)-3-氰基-4-羟基-5-(羟甲基)氧杂环戊-2-基]-2-氧代嘧啶-4-基]十六酰胺

nucleoside analog

Concentrations of Sapacitabine required to achieve an IC ₅₀ range from 3±0.6 μM for the colon cancer cell line HCT116 to 67±14 μM 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 G ₂ /M phase. L1210 cells with deoxycytidine kinase (dCK) activity are sensitive to Sapacitabine, (IC ₅₀ 20±6 μM). In the docetaxel/Sapacitabine combinations, synergistic effects (CI<1) are observed when docetaxel is given before Sapacitabine in both cell lines.

On Day 14, the Sapacitabine (5 mg/kg)+vorinostat (33 mg/kg) group has a mean tumour volume of 245 mm ³ 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 mm ³ and a TGI of 112%.