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
| 中文名称 | 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 |
|---|---|
| 中文同义词 | 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;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;沙帕他滨;化合物SAPACITABINE |
| 英文名称 | Sapacitabine |
| 英文同义词 | N-[1-[(2R,3S,4S,5R)-3-cyano-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-2- oxo-pyrimidin-4-yl]hexadecanamide;Sapacitabine;1-(2-C-Cyano-2-deoxy-β-D-arabino-pentofuranosyl)cytosine;1-(2-Deoxy-2-cyano-β-D-arabinofuranosyl)cytosine;4-Amino-1-[(3β-cyano-4α-hydroxy-5β-hydroxymethyltetrahydrofuran)-2β-yl]pyrimidin-2(1H)-one;CNDAC;1-(2-cyano-2-deoxy-β-D-arabinofuranosyl)-4-(palMitoylaMino)pyriMidin-2(1H)-one,Sapacitabine;2'-cyano-2'-deoxy-N4-palMitoyl-1-β-D-arabinofuranosyl-cytosine, sapacitabine, CYC682 |
| CAS号 | 151823-14-2 |
| 分子式 | C26H42N4O5 |
| 分子量 | 490.64 |
| EINECS号 | |
| 相关类别 | 核苷类 |
| Mol文件 | 151823-14-2.mol |
| 结构式 | ![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 结构式](CAS/GIF/151823-14-2.gif) |
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 性质
| 熔点 | >177°C (dec.) |
|---|---|
| 密度 | 1.21±0.1 g/cm3(Predicted) |
| 储存条件 | -20°C Freezer, Under inert atmosphere |
| 溶解度 | 可溶于DMSO（轻微）、甲醇（轻微、加热） |
| 酸度系数(pKa) | 10.04±0.20(Predicted) |
| 形态 | 固体 |
| 颜色 | 白色至类白色 |
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%.
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/16 | HY-16445 | 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 Sapacitabine | 151823-14-2 | 5mg | 750元 |
| 2024/01/16 | HY-16445 | 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 Sapacitabine | 151823-14-2 | 10mM * 1mLin DMSO | 810元 |