(E)-2'-DEOXY-2'-(FLUOROMETHYLENE) CYTIDINE
- CAS号:130306-02-4
- 英文名:(E)-2'-DEOXY-2'-(FLUOROMETHYLENE) CYTIDINE
- 中文名:(E)-2'-DEOXY-2'-(FLUOROMETHYLENE) CYTIDINE
- CBNumber:CB3221204
- 分子式:C10H12FN3O4
- 分子量:257.22
- MOL File:130306-02-4.mol
- 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; Need ultrasonic)
- 形态 :Solid
- 酸度系数(pKa) :12.50±0.60(Predicted)
- 颜色 :Off-white to light yellow
(E)-2'-DEOXY-2'-(FLUOROMETHYLENE) CYTIDINE性质、用途与生产工艺
- 生物活性 Tezacitabine 是一种具有细胞生长抑制和细胞毒性的抗代谢药,是一种核苷类似物。Tezacitabine 不可逆地抑制核糖核苷酸还原酶 (ribonucleotide reductase) 并干扰 DNA 复制和修复。Tezacitabine 有效诱导细胞凋亡 (apoptotic),可用于白血病和实体瘤的研究。
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靶点
Ribonucleotide reductase
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体外研究
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. -
体内研究
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.
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