Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Tezacitabine 是一种抑制细胞生长和细胞毒性的抗代谢物。 Tezacitabine 是一种核苷类似物,具有双重作用机制。 Tezacitabine 不可逆地抑制核糖核苷酸还原酶,并可在复制或修复过程中掺入 DNA,导致 DNA 链终止。 Tezacitabine 在细胞周期的 G1 期和 S 期阻断肿瘤细胞并诱导凋亡细胞死亡。 Tezacitabine 具有治疗白血病和实体瘤的潜力[1][2]。
产品描述 | Tezacitabine is a cytostatic and cytotoxic antimetabolite. Tezacitabine is a nucleoside analogue characterized by a dual mechanism of action. Tezacitabine irreversibly inhibits ribonucleotide reductase and can be incorporated into DNA during replication or repair, resulting in DNA chain termination. Tezacitabine blocks tumor cells in G1 and S phases of the cell cycle and induces apoptotic cell death. Tezacitabine has the potential to treat leukemia and solid tumors[1][2]. |
体外活性 | Tezacitabine (0.01-10 μM; 24 hours; CCRF-SB, KG-1, Jurkat, COLO-205, MCF-7 and PC-3 cells) treatment leads to the G1 and S-phase leaky block of the cell cycle [1]. Tezacitabine (0.01-10 μM; 24 hours; CCRF-SB, KG-1, Jurkat, COLO-205, MCF-7 and PC-3 cells) treatment concentration-dependently apoptosis the cells by the caspase 3/7 pathway[1]. Tezacitabine has highly cytostatic and cytotoxic properties. The cytotoxic effect of tezacitabine is manifested not only in apoptosis but also in changes in protein metabolism[1]. Cell Cycle Analysis [1] 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 leaky block of the G1 (at concentrations higher than 10 nM) and S-phase (at low concentration) of the cell cycle. Apoptosis Analysis [1] 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: Concentration-dependently induced apoptotic death of cells by the caspase 3/7 pathway. |
体内活性 | Tezacitabine (100 mg/kg; intraperitoneal injection; daily; female nude mice) treatment inhibits the growth of tumors in HCT 116 tumor xenografts [2]. Animal Model: Female nude mice (7-9-week-old) injected with HCT 116 cells [2] Dosage: 100 mg/kg Administration: Intraperitoneal injection; daily; 14 days Result: Tumor growth in HCT 116 tumor xenografts is inhibited. |
分子量 | 257.22 |
分子式 | C10H12FN3O4 |
CAS No. | 130306-02-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Tezacitabine 130306-02-4 Inhibitor inhibitor inhibit