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Ko 143 is a potent and selective inhibitor of BCRP, preventing the export of mitoxantrone and topotecan in breast cancer cell lines (EC50s = 23 and 26 nM, respectively).1 It is much less effective at the transporters P-
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1. Potent and specific inhibition of the breast cancer resistance protein multidrug transporter in vitro and in mouse intestine by a novel analogue of fumitremorgin C. Mol. Cancer Ther. 1(6), 417-425 (2002).
2. A novel PET protocol for visualization of breast cancer resistance protein function at the blood-