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CAS No.: 3690-10-6

泽布拉林 Catalog No. CSN12234

Synonyms: NSC309132;4-Deoxyuridine

Zebularine is a DNA methylation inhibitor which forms a covalent complex with DNA methyltransferases, it also inhibits cytidinedeaminase with Ki of 2 μM.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Cytidine Deaminase

Ki:2μM
描述The DNA methyltransferase (DNMT) family are enzymes that can mediate the DNA methylation. Inhibiting the DNMTs have shown particular promise in reducing the formation of tumors^[6]. Zebularine is a second-generation inhibitor of DNMT with IC50 value of 95 nM on DNMT1^[7]. The TFK-1 and HuCCT1 cells were treated with zebularine from 100 - 1000 µM for 72 hours. The cell viability was significantly reduced in a dose dependent manner measured by WST assay. The protein expression level of DNMT1, DNMT3a, DNMT3b examined by western blotting assay was significantly inhibited for both cell lines at concentration of 400 µM and above^[8]. BALB/c nude mice with tumor were treated with 10, 50 and 100 mg/kg zebularine via oral gavage in a solution of 0.45% saline every four days for 20 days. The tumor growth was reduced in a dose dependent manner and the cell death in the tumor mass via apoptosis was induced by the treatement of zebularine as measured by the TUNEL assay^[9].
作用机制Zebularine could form tight covalent complexes between the DNMT proteins and zebularine-substitute DNA^[10].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
human HCT15 cells	100 μM	Function assay	8 days	Induction of p16 gene expression in human HCT15 cells at 100 uM after 8 days by real time PCR in presence of 100 mM thymidine	19006382
human T24 cells	100 μM	Function assay	8 days	Induction of p16 gene expression in human T24 cells at 100 uM after 8 days by real time PCR in presence of 100 mM thymidine	19006382

动物研究

剂量

Mice: 500 mg/kg^[3] (i.p.); 100 mg/kg^[4] (i.v.); 1000 mg/kg^[4] (p.o.) Dog: 4 mg/kg, 8 mg/kg^[5] (p.o.)

给药途径

i.p., i.v., p.o.

动物药代数据

Animal	Mice^[4]	Rats^[4]	Monkeys^[4]
Dose	100 mg/kg (i.v.) 1000 mg/kg (p.o.)	50 mg/kg (i.v.) 250 mg/kg (p.o.)	500 mg/kg
Administration	i.v. p.o.	i.v. p.o.	i.v. or p.o.
F	6.7% (p.o.)	3.1% (p.o.)	0.1% (p.o.)
T_1/2	40 min (i.v.)	363 min (i.v.)	70 min (i.v.)
AUC	7323 g/ml·min (i.v.) 4935 g/ml·min (p.o.)	12526 g/ml·min (i.v.) 1969 g/ml·min (p.o.)	88020 g/ml·min (i.v.) 84 g/ml·min (p.o.)
CL_app	203 ml/min/kg (p.o.)	127 ml/min/kg (p.o.)	6021 ml/min/kg (p.o.)
CL_tb	13.65 ml/min/kg (i.v.)	3.99 ml/min/kg (i.v.)	5.68 ml/min/kg (i.v.)

参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 4.3821 mL
- 21.9104 mL
- 43.8208 mL
- 5 mM
- 0.8764 mL
- 4.3821 mL
- 8.7642 mL
- 10 mM
- 0.4382 mL
- 2.1910 mL
- 4.3821 mL

技术信息

CAS号

3690-10-6

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C9H12N2O5

运输

蓝冰

分子量

228.20

别名

NSC309132;4-Deoxyuridine

溶解度

DMSO	44.0 mg/mL (192.8 mM)
Water	44.0 mg/mL (192.8 mM)
Ethanol	Insoluble

动物实验配方

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