Sapacitabine
Sapacitabine
CAS: 151823-14-2
Molecular Formula: C26H42N4O5
Sapacitabine - Names and Identifiers
Sapacitabine - Physico-chemical Properties
| Molecular Formula | C26H42N4O5 |
| Molar Mass | 490.64 |
| Density | 1.21±0.1 g/cm3(Predicted) |
| Melting Point | >177°C (dec.) |
| Solubility | DMSO (Slightly), Methanol (Slightly, Heated) |
| Appearance | Solid |
| Color | White to Off-White |
| pKa | 10.04±0.20(Predicted) |
| Storage Condition | -20°C Freezer, Under inert atmosphere |
| In vitro study | 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. |
| In vivo study | 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%. |
Sapacitabine - Reference Information
| biological activity | Sapacitabine are orally available nucleoside analog prodrugs and are structurally related to cytarabine. |
| target | nucleoside analog |
| in vitro study | Concentrations of Sapacitabine required to achieve an IC 50 range from 3±0.6 μ m for the colon cancer cell line HCT116 to 67±14 μ m 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. |
| in vivo study | 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 0mm 3 and a TGI of 112%. |
Last Update：2024-04-09 18:58:34
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