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• 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： -20℃

• 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

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *