Sapacitabine is an orally availablenucleoside analogprodrug that is structurally related to cytarabine.

nucleoside analog^[1]

Concentrations of Sapacitabine required to achieve an IC₅₀range 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 G₂/M phase. L1210 cells with deoxycytidine kinase (dCK) activity are sensitive to Sapacitabine, (IC₅₀20±6 μM). 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 mm³and 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 mm³and a TGI of 112%^[2].

490.64

Solid

C₂₆H₄₂N₄O₅

151823-14-2

Room temperature in continental US; may vary elsewhere.

DMSO : 33.33 mg/mL(67.93 mM;Need ultrasonic)

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