Drug name: Irinotecan + YHO-13351

Cas.no	PubChem ID
97682-44-5	60838

Known Target
DNA topoisomerase 1	P11387
DNA topoisomerase I, mitochondrial	Q969P6
Structure
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Introduction
Irinotecan is an antineoplastic enzyme inhibitor primarily used in the treatment of colorectal cancer. It is a derivative of camptothecin that inhibits the action of topoisomerase I. Irinotecan prevents religation of the DNA strand by binding to topoisomerase I-DNA complex, and causes double-strand DNA breakage and cell death. It is a derivative of camptothecin.

Cas.no	PubChem ID
912288-64-3

Known Target
ATP-binding cassette sub-family G member 2	Q9UNQ0
Structure
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Introduction
An in vivo bioavailable and highly water soluble ( >100 mg/ml) diethylaminoacetate prodrug of YHO-13177 that reverses ABCG2-mediated irinotecan resistance in P388/BCRP and HCT116/BCRP xenograft mouse models, and suppresses tumor growth and significantly enhances the survival (100 or 200 mg/kg, i.p.).

• [1] ABCG2 inhibitor YHO-13351 sensitizes cancer stem/initiating-like side population cells to irinotecan. Shishido, Y., et al. (2013).Anticancer Res.33(4):1379-86.
  23564776. [ 23564776 ]
• [2] Novel acrylonitrile derivatives, YHO-13177 and YHO-13351, reverse BCRP/ABCG2-mediated drug resistance in vitro and in vivo. Yamazaki, R., et al. (2011).Mol Cancer Ther.10(7):1252-63.
  21566063. [ 21566063 ]