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YHO-13177

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Chemical Structure| 912287-56-0 同义名 : -
CAS号 : 912287-56-0
货号 : A407213
分子式 : C20H22N2O3S
纯度 : 99%+
分子量 : 370.465
MDL号 : MFCD28900680
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(94.48 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Breast cancer resistance protein (BCRP) is a member of the ATP-binding cassette (ABC) transporter superfamily that regulates drug resistance. YHO-13177 is a novel acrylonitrile derivative that has been shown to reverse BCRP-mediated drug resistance both in vitro and in vivo. In BCRP-transduced HCT116 cells, treatment with YHO-13177 at 0.01-1 μM reversed the drug resistance to BCRP substrates (SN-38, topotecan, and mitoxantrone) in a dose-dependent manner, while it showed no effect on the drug sensitivity of parental HCT116 cells expressing no BCRP. YHO-13177 at the concentrations of 0.01-1 μM also reversed the drug resistance in A549 cells with BCRP-mediated acquired resistance to SN-38. The cytotoxicity of SN-38 in cells that intrinsically express BCRP (RPMI-8226, NCI-H23, NCI-H460, and AsPC-1 cell lines) was significantly potentiated by YHO-13177 at 0.01-1 μM. Treatment with YHO-13177 (0.1 to 10 μM) significantly induced the intracellular accumulation of Hoechst 33342 in both A549/SN4 and HCT116/BCRP cells. YHO-13177 from 0.01-1 μM partially suppressed the expression of BCRP protein in both A549/SN4 and HCT116/BCRP cells without affecting the mRNA expression of BCRP. In mice inoculated with BCRP-transduced murine leukemia P388 cells, the combined treatment of irinotecan (i.v., 45 mg/kg) and YHO-13351 (p.o., 50, 100, or 200 mg/kg), a prodrug of YHO-13177, significantly enhanced the survival time of mice in a dose-dependent manner[2].
作用机制 YHO-13177 is a novel acrylonitrile derivative that reverses the drug resistance and enhances the cytotoxicity of anticancer drugs in BCRP-expressing cancer cells and xenografts by inhibiting the drug transport function and the posttranscriptional expression of BCRP.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.70mL

0.54mL

0.27mL

13.50mL

2.70mL

1.35mL

26.99mL

5.40mL

2.70mL
参考文献

[1]Yamazaki R, Nishiyama Y, 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.

[2]Yamazaki R, Nishiyama Y, Furuta T, Hatano H, Igarashi Y, Asakawa N, Kodaira H, Takahashi H, Aiyama R, Matsuzaki T, Yagi N, Sugimoto Y. 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. doi: 10.1158/1535-7163.MCT-10-0874. Epub 2011 May 12. PMID: 21566063.