912287-56-0
Chemical Structure
YHO-13177
- CAS. Nr.: 912287-56-0
- Formula:C20H22N2O3S
- Molecular Weight:370.47
IUPAC Name: (Z)-2-(3,4-dimethoxyphenyl)-3-(5-(4-hydroxypiperidin-1-yl)thiophen-2-yl)acrylonitrile
InChIKey: NOGGBVNCVONHHC-RVDMUPIBSA-N
SMILES: N#C/C(C1=CC=C(OC)C(OC)=C1)=C\C2=CC=C(N3CCC(O)CC3)S2
Biological Activity: YHO-13177, a acrylonitrile derivative, is an orally active, potent and specific inhibitor of breast cancer resistance protein (BCRP) and ABCG2 with an IC50 value of 10 nM. YHO-13177 potentiates the cytotoxicity of SN-38 in HCT116 and A549 cells that express BCRP. YHO-13177 combined with Irinotecan (HY-16562) significantly suppresses the tumor growth in an HCT116/BCRP xenograft model[1][2][3].
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YHO-13177 | 99.65% | YHO-13177, a acrylonitrile derivative, is an orally active, potent and specific inhibitor of breast cancer resistance protein (BCRP) and ABCG2 with an IC50 value of 10 nM. YHO-13177 potentiates the cytotoxicity of SN-38 in HCT116 and A549 cells that express BCRP. YHO-13177 combined with Irinotecan (HY-16562) significantly suppresses the tumor growth in an HCT116/BCRP xenograft model. | ||||||||||||||||||||
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- [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. [Content Brief]
- [2]. Shishido Y, et al. ABCG2 inhibitor YHO-13351 sensitizes cancer stem/initiating-like side population cells to irinotecan. Anticancer Res. 2013 Apr;33(4):1379-86. [Content Brief]
- [3]. Yu S, et al. The mechanisms of multidrug resistance of breast cancer and research progress on related reversal agents. Bioorg Med Chem. 2023 Nov 15;95:117486. [Content Brief]
Keywords
