中文名 | 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 |
英文名 | Sapacitabine |
别名 | 沙帕他滨 化合物SAPACITABINE N-[1-(2-氰基-2-脱氧-Β-D-阿拉伯呋喃糖基)-1,2-二氢-2-氧代-4-嘧啶基]十六烷酰胺 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 |
英文别名 | CNDAC Sapacitabine 1-(2-Deoxy-2-cyano-β-D-arabinofuranosyl)cytosine 1-(2-C-Cyano-2-deoxy-β-D-arabino-pentofuranosyl)cytosine 2'-cyano-2'-deoxy-N4-palMitoyl-1-β-D-arabinofuranosyl-cytosine, sapacitabine, CYC682 4-Amino-1-[(3β-cyano-4α-hydroxy-5β-hydroxymethyltetrahydrofuran)-2β-yl]pyrimidin-2(1H)-one 1-(2-cyano-2-deoxy-β-D-arabinofuranosyl)-4-(palMitoylaMino)pyriMidin-2(1H)-one,Sapacitabine N-[1-[(2R,3S,4S,5R)-3-cyano-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-2- oxo-pyrimidin-4-yl]hexadecanamide |
CAS | 151823-14-2 |
化学式 | C26H42N4O5 |
分子量 | 490.64 |
密度 | 1.21±0.1 g/cm3(Predicted) |
熔点 | >177°C (dec.) |
溶解度 | DMSO (微溶),甲醇 (微溶,加热) |
酸度系数 | 10.04±0.20(Predicted) |
存储条件 | -20°C Freezer, Under inert atmosphere |
外观 | 固体 |
颜色 | White to Off-White |
体外研究 | 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. |
体内研究 | 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%. |
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