tcsc0298 Ko 143

Ko 143 is a practical breast cancer resistance protein multidrug transporter inhibitor BCRP, with the EC₉₀ value of 26 nM.

IC50 & Target: EC90: 26 nM (BCRP)

In Vitro: Ko143 (10 nM) significantly decreases (2.5-fold) the IC₅₀ of MTX for HEK G2 cells and mouse G2 cells. Ko143 (1-100 μM) metabolite does not inhibit the function of ABC Transporters^[1]. Reversal of drug resistance in topotecan-selected mouse MEF3.8/T6400 cells and human IGROV1/T8 cells by FTC analogue Ko143. Ko143 is applied at zero, one, or eight times the EC₉₀ concentration of 25 nM^[2]. Ko143 inhibits BCRP-mediated transport of rosuvastatin in Madin-Darby Canine Kidney (MDCK) 2-BCRP421CC (wild type) cells and MDCK2-BCRP421AA (mutant type) cells^[3].

In Vivo: Ko143 (10 mg/kg, p.o.) increases the oral availability of topotecan in mice^[2]. Ko143 significantly affects the pharmacokinetics of rosuvastatin in rats^[3].