(E)-2'-DEOXY-2'-(FLUOROMETHYLENE) CYTIDINE
(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 |
(E)-2'-DEOXY-2'-(FLUOROMETHYLENE) CYTIDINE 用途与合成方法
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. |