货号	规格	价格	上海	北京	珠海	重庆	武汉
S87203-5mg促销	99.70%	￥300.00 ￥240.00 S87203-5mg ￥240.00 现货	6 6	-	-	-	-
S87203-10mg促销	99.70%	￥440.00 ￥352.00 S87203-10mg ￥352.00 现货	6 6	-	-	-	-
S87203-25mg促销	99.70%	￥540.00 ￥486.00 S87203-25mg ￥486.00 现货	5 5	-	-	-	-
S87203-100mg	≥99%	￥910.00 S87203-100mg ￥910.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

YHO-13177 is a potent and specific inhibitor of BCRP; potentiated the cytotoxicity of SN-38 in cancer cells and no effect on P-glycoprotein–mediated paclitaxel resistance in MDR1-transduced human leukemia K562 cells. IC50 value: Target: BCRP inhibitor in vitro: YHO-13177 potentiated the cytotoxicity of SN-38, mitoxantrone, and topotecan in both BCRP-transduced human colon cancer HCT116 (HCT116/BCRP) cells and SN-38–resistant human lung cancer A549 (A549/SN4) cells that express BCRP, but had little effect in the parental cells. In addition, YHO-13177 potentiated 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. In contrast, it had no effect on P-glycoprotein–mediated paclitaxel resistance in MDR1-transduced human leukemia K562 cells and multidrug resistance-related protein 1–mediated doxorubicin resistance in MRP1-transfected human epidermoid cancer KB-3-1 cells. YHO-13177 increased the intracellular accumulation of Hoechst 33342, a substrate of BCRP, at 30 minutes and partially suppressed the expression of BCRP protein at more than 24 hours after its treatment in both HCT116/BCRP and A549/SN4 cells [1]. in vivo: In mice, YHO-13351 was rapidly converted into YHO-13177 after its oral or intravenous administration. 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

靶点：

BCRP

体内研究：

YHO-13177 (19.7 μM, 静脉注射，或 27.3 μM, 口服，单次剂量，25 天) 是由 YHO-13351 转换的，增加 BCRP 转导的小鼠白血病 P388 细胞接种小鼠的存活时间，抑制 HCT116/BCRP 异种移植小鼠模型中的肿瘤生长。

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	2.699 ml	13.497 ml	26.993 ml
5 mM	0.54 ml	2.699 ml	5.399 ml
10 mM	0.27 ml	1.35 ml	2.699 ml
50 mM	0.054 ml	0.27 ml	0.54 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。

参考文献

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