(E)-2'-DEOXY-2'-(FLUOROMETHYLENE) CYTIDINE
| 中文名称 | (E)-2'-DEOXY-2'-(FLUOROMETHYLENE) CYTIDINE |
|---|---|
| 中文同义词 | 替扎西他滨;化合物 TEZACITABINE |
| 英文名称 | (E)-2'-DEOXY-2'-(FLUOROMETHYLENE) CYTIDINE |
| 英文同义词 | (E)-2'-DEOXY-2'-(FLUOROMETHYLENE) CYTIDINE;tezaciabine;Cytidine, 2'-deoxy-2'-(fluoromethylene)-, (2'E)-;2'-deoxy-2'-(fluoromethylene)-(2E)Cytidine |
| CAS号 | 130306-02-4 |
| 分子式 | C10H12FN3O4 |
| 分子量 | 257.22 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 130306-02-4.mol |
| 结构式 |  |
(E)-2'-DEOXY-2'-(FLUOROMETHYLENE) CYTIDINE 性质
| 沸点 | 512.5±60.0 °C(Predicted) |
|---|---|
| 密度 | 1.71±0.1 g/cm3(Predicted) |
| 储存条件 | -80°C |
| 溶解度 | DMSO：200 mg/mL（777.54 mM；需要超声波） |
| 形态 | 固体 |
| 酸度系数(pKa) | 12.50±0.60(Predicted) |
| 颜色 | 米白色至浅黄色 |
Ribonucleotide reductase
Tezacitabine (0.01-10 µM; 24 hours; CCRF-SB, KG-1, Jurkat, COLO-205, MCF-7 and PC-3 cells) treatment induces the G1 and S-phase leaky block of the cell cycle.
Tezacitabine (0.01-10 µM; 24 hours; CCRF-SB, KG-1, Jurkat, COLO-205, MCF-7 and PC-3 cells) treatment apoptotic death of cells by the caspase 3/7 pathway in a concentration-dependent manner.
Tezacitabine has strong cytostatic and cytotoxic properties. Cytotoxic effect of Tezacitabine reveals not only as apoptosis, but also as a change in protein metabolism.
Cell Cycle Analysis
| Cell Line: | CCRF-SB, KG-1, Jurkat, COLO-205, MCF-7 and PC-3 cells |
| Concentration: | 0.01 µM, 0.1 µM, 1.0 µM, and 10 µM |
| Incubation Time: | 24 hours |
| Result: | Induced the G1 (at concentrations higher than 10 nM) and S-phase (at low concentration) leaky block of the cell cycle. |
Apoptosis Analysis
| Cell Line: | CCRF-SB, KG-1, Jurkat, COLO-205, MCF-7 and PC-3 cells |
| Concentration: | 0.01 µM, 0.1 µM, 1.0 µM, and 10 µM |
| Incubation Time: | 24 hours |
| Result: | Induced apoptotic death of cells by the caspase 3/7 pathway in a concentration-dependent manner. |
Tezacitabine (100 mg/kg; intraperitoneal injection; daily; female nude mice) treatment inhibits tumor growth in HCT 116 tumor xenografts.
| Animal Model: | Female nude mice (7-9-week-old) injected with HCT 116 cells |
| Dosage: | 100 mg/kg |
| Administration: | Intraperitoneal injection; daily; 14 days |
| Result: | Inhibited tumor growth in HCT 116 tumor xenografts. |