1346753-00-1
Chemical Structure
YHO-13351
- CAS No.: 1346753-00-1
- Formula:C27H37N3O7S2
- Molecular Weight:579.73
IUPAC Name: (Z)-1-(5-(2-cyano-2-(3,4-dimethoxyphenyl)vinyl)thiophen-2-yl)piperidin-4-yl diethylglycinate methanesulfonate
InChIKey: XOEIHKAPFXUACW-QMGGKDRNSA-N
SMILES: N#C/C(C1=CC=C(OC)C(OC)=C1)=C\C2=CC=C(N3CCC(OC(CN(CC)CC)=O)CC3)S2.O=S(C)(O)=O
Biological Activity: YHO-13351 is an orally active ABCG2 inhibitor. YHO-13351 modulates the function of ABCG2, blocks BCRP-mediated compound efflux, downregulates the expression of breast cancer resistance protein at the post-transcriptional level, and reverses ABCG2-associated tolerance. YHO-13351 restores the toxicity of SN-38 to SN-38-resistant cancer cells and sensitizes cancer cells to Irinotecan. YHO-13351 is a water-soluble prodrug that is rapidly converted to YHO-13177 (HY-12757) in mice. YHO-13351 prolongs the median survival time of mice bearing cancer cell xenografts when combined with IMMU-132. YHO-13351 extends the survival time of tumor-bearing mice and inhibits the growth of xenograft tumors when combined with Irinotecan. YHO-13351 can be used for the research of breast cancer, gastric cancer, BCRP-mediated drug-resistant cancers, and cervical cancer[1][2][3].
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YHO-13351 | 99.16% | YHO-13351 is an orally active ABCG2 inhibitor. YHO-13351 modulates the function of ABCG2, blocks BCRP-mediated compound efflux, downregulates the expression of breast cancer resistance protein at the post-transcriptional level, and reverses ABCG2-associated tolerance. YHO-13351 restores the toxicity of SN-38 to SN-38-resistant cancer cells and sensitizes cancer cells to Irinotecan. YHO-13351 is a water-soluble prodrug that is rapidly converted to YHO-13177 (HY-12757) in mice. YHO-13351 prolongs the median survival time of mice bearing cancer cell xenografts when combined with IMMU-132. YHO-13351 extends the survival time of tumor-bearing mice and inhibits the growth of xenograft tumors when combined with Irinotecan. YHO-13351 can be used for the research of breast cancer, gastric cancer, BCRP-mediated drug-resistant cancers, and cervical cancer. | ||||||||||||||||||||
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- [1]. Chang CH, et al. Combining ABCG2 Inhibitors with IMMU-132, an Anti-Trop-2 Antibody Conjugate of SN-38, Overcomes Resistance to SN-38 in Breast and Gastric Cancers. Mol Cancer Ther. 2016;15(8):1910-1919. [Content Brief]
- [2]. 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;10(7):1252-1263. [Content Brief]
- [3]. Shishido Y, et al. ABCG2 inhibitor YHO-13351 sensitizes cancer stem/initiating-like side population cells to irinotecan. Anticancer Res. 2013;33(4):1379-1386. [Content Brief]
Keywords
