產(chǎn)品描述: | Zebularine (NSC309132; 4-Deoxyuridine) is a DNA methyltransferase inhibitor. Zebularine also inhibits cytidine deaminase with a Ki of 0.95 μM. |
靶點(diǎn): |
DNMT1;DNMT3a/3L;Cytidine deaminase:0.95 μM (Ki);Autophagy ;DNAMethyltransferase;Autophagy |
體內(nèi)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 |
參考文獻(xiàn): |
1. Champion C, et al. Mechanistic insights on the inhibition of c5 DNA methyltransferases by zebularine. PLoS One. 2010 Aug 24;5(8):e12388. 2. Cheng JC, et al. Inhibition of DNA methylation and reactivation of silenced genes by zebularine. J Natl Cancer Inst. 2003 Mar 5;95(5):399-409. 3. Billam M, et al. Effects of a novel DNA methyltransferase inhibitor zebularine on human breast cancer cells. Breast Cancer Res Treat. 2010 Apr;120(3):581-92. 4. Lemaire M, et al. Inhibition of cytidine deaminase by zebularine enhances the antineoplastic action of 5-aza-2'-deoxycytidine. Cancer Chemother Pharmacol. 2009 Feb;63(3):411-6. |
溶解性: |
Soluble in DMSO、H2O |
保存條件: |
2-8℃ |
配置溶液濃度參考: |
|
1mg |
5mg |
10mg |
1 mM |
4.382 ml |
21.911 ml |
43.821 ml |
5 mM |
0.876 ml |
4.382 ml |
8.764 ml |
10 mM |
0.438 ml |
2.191 ml |
4.382 ml |
50 mM |
0.088 ml |
0.438 ml |
0.876 ml |
|
注意: |
部分產(chǎn)品我司僅能提供部分信息,我司不保證所提供信息的權(quán)威性,僅供客戶參考交流研究之用。 |