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包装规格：250mg in glass bottle
溶解性：溶于DMSO（≥ 100 mg/mL）
产品描述：基本信息 产品编号：Z10042 产品名称：Zebularine CAS: 3690-10-6   储存条件 粉末 -20℃ 四年     分子式： C9H12N2O5 溶于液体 -80℃ 六个月 分子量： 228.20 -20℃ 一个月 化学名：      Solubility (25°C)   体外 DMSO 46mg/mL (201.57mM) Ethanol Insoluble Water 46mg/mL (201.57mM) 体内（现配现用） Saline 30mg/mL ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 4.3821mL 21.9106mL 43.8212mL 5mM 0.8764mL 4.3821mL 8.7642mL 10mM 0.4382mL 2.1911mL 4.3821mL 50mM 0.0876mL 0.4382mL 0.8764mL   生物活性 产品描述 是DNA甲基转移酶抑制剂；也可抑制胞苷脱氨酶，Ki值为0.95μM。 靶点/IC50 DNA methyltransferase(Cell-free assay) Cytidine deaminase(Cell-free assay)   2μM(Ki)   体外研究 Zebularine exerts its demethylation activity by stabilizing the binding of DNMTs to DNA,hindering the methylation and decreasing the dissociation, thereby trapping the enzyme and preventing turnover even at other sites. zebularine enhances tumor cell chemo- and radiosensitivity and has antimitogenic and angiostatic activities.Zebularine inhibits DNA methylation and reactivates a gene previously silenced by methylation.Zebularine induces the myogenic phenotype in 10T1/2 cells,which is a phenomenon unique to DNA methylation inhibitors.Zebularine reactivates a silenced p16 gene and demethylated its promoter region in T24 bladder carcinoma cells.Zebularine treatment inhibits cell growth in a dose and time dependent manner with an IC50 of -100μM and 150μM in MDA-MB-231 and MCF-7 cells,respectively,on 96h exposure.At high doses zebularine induced changes in apoptotic proteins in a cell line specific manner manifested by alteration in caspase-3,Bax,Bcl2 and PARP cleavage.Zebularine is also a potent competitive inhibitor of the enzyme CR deaminase.The Ki for zebularine is 0.95μM. 体内研究 Zebularine is only slightly cytotoxic to tumor-bearing mice.Compared with those in control mice,tumor volumes are statistically significantly reduced in mice treated with high-dose zebularine administered by intraperitoneal injection or by oral gavage.Zebularine also enhances the survival time of mice with L1210 leukemia treated with 5-AZA-CdR.About 27% of the mice treated with this drug combination has a survival time longer than the mice treated with only 5-AZA-CdR.   推荐实验方法(仅供参考) 细胞实验: For methylation analysis,10T1/2 cells and T24 cells are treated with the various concentrations of zebularine.For 10T1/2 cells,the medium is changed 24 hours after the initial drug treatment,whereas for T24 cells,the medium is changed 24 hours or 48 hours after the initial drug treatment.DNA and RNA are harvested from 10T1/2 cells 72 hours after initial drug treatment and from T24 cells 96 hours after initial drug treatment.The methylation status of the indicated DNA regions is measured in two separate and independent experiments, both of which are done in duplicate.   动物实验:   EJ6 cells (5×105/injection) suspended in PBS are inoculated subcutaneously into the right and left flanks (along the midaxillary lines) of 4- to 6-week-old male BALB/c nu/nu mice.Mice (n=30) are randomLy divided into six groups (intraperitoneal control,oral control,intraperitoneal zebularine at 500mg/kg,oral zebularine at 500mg/kg,intraperitoneal zebularine at 1000mg/kg,and oral zebularine at 1000mg/kg).Each group consisted of five mice (at least six tumors per group;one or two mice per group are randomLy killed at earlier time points to establish a time course of expression).After 2–3 weeks and after macroscopic tumors (50–200 mm3) had formed,zebularine or control treatments are initiated.Zebularine, at doses of 500mg/kg or 1000mg/kg,is administered daily by intraperitoneal injection or oral gavage in a solution of 0.45% saline over a period of 18 days.
保存条件：-20℃

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