An in vivo bioavailable (~87%; t1/2 <5 mins. during p.o. and i.v. administration) and highly water soluble ( >100mg/ml) diethylaminoacetate prodrug of YHO-13177 that reverses BCRP-mediated irinotecan resistance in P388/BCRP and HCT116/BCRP xenograft mouse models, and suppresses tumor growth and significantly enhances the survival (100 or 200mg/kg, i.p.).