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。
生物活性
Tezacitabine is a cytostatic and cytotoxic antimetabolite and a nucleoside analogue. Tezacitabine irreversibly inhibits the ribonucleotide reductase and interferes with DNA replication and repair. Tezacitabine effectively induces cells apoptotic. Tezacitabine has the potential for leukemias and solid tumors (carcinomas) treatment.
性状
Solid
IC50 & Target[1][2]
Ribonucleotide reductase
体外研究(In Vitro)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Tezacitabine (100 mg/kg; intraperitoneal injection; daily; female nude mice) treatment inhibits tumor growth in HCT 116 tumor xenografts. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-80°C
ClinicalTrial
参考文献
[1]. Janusz S Skierski, et al. Tezacitabine Blocks Tumor Cells in G1 and S Phases of the Cell Cycle and Induces Apoptotic Cell Death. Acta Pol Pharm. May-Jun 2005;62(3):195-205.[2]. Pietro Taverna, et al. Tezacitabine Enhances the DNA-directed Effects of Fluoropyrimidines in Human Colon Cancer Cells and Tumor Xenografts. Biochem Pharmacol. 2007 Jan 1;73(1):44-55.
溶解度数据
In Vitro: H2O : 200 mg/mL (777.54 mM; Need ultrasonic)DMSO : 200 mg/mL (777.54 mM; Need ultrasonic)配制储备液