| 产品描述： | YHO-13351 is the water-soluble prodrug of YHO-13177, which is a potent and specific BCRP inhibitor |
| 靶点： |
Epigenetic Reader Domain;EpigeneticReaderDomain |
| 体外研究： |
YHO-13177 enhances SN-38, mitoxantrone and topotecan in BCRP transduced human colon cancer HCT116 (HCT116/BCRP) cells and BCRP-expressing SN-38 resistant human lung cancer A549 (A549/SN4) Cytotoxicity in cells, but little effect on parental cells. In addition, YHO-13177 potentiates the cytotoxicity of SN-38 in human lung cancer NCI-H460 and NCI-H23, myeloma RPMI-8226, and pancreatic cancer AsPC-1 cells that intrinsically expressed BCRP. YHO-13177 increases the intracellular accumulation of Hoechst 33342, a substrate of BCRP, at 30 minutes and partially suppresses the expression of BCRP protein at more than 24 hours after its treatment in both HCT116/BCRP and A549/SN4 cells . |
| 体内研究： |
YHO-13351 was rapidly converted into YHO-13177 after its oral or intravenous administration In mice. Coadministration of irinotecan with YHO-13351 significantly increased the survival time of mice inoculated with BCRP-transduced murine leukemia P388 cells and suppressed the tumor growth in an HCT116/BCRP xenograft model, whereas irinotecan alone had little effect in these tumor models |
| 参考文献： |
1. Yamazaki R, et al. Novel acrylonitrile derivatives, YHO-13177 and YHO-13351, reverse BCRP/ABCG2-mediated drug resistance in vitro and in vivo. Mol Cancer Ther. 2011 Jul;10(7):1252-63. |
| 溶解性： |
soluble in DMSO |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.725 ml |
8.625 ml |
17.249 ml |
| 5 mM |
0.345 ml |
1.725 ml |
3.45 ml |
| 10 mM |
0.172 ml |
0.862 ml |
1.725 ml |
| 50 mM |
0.034 ml |
0.172 ml |
0.345 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
