The biotin-attached G8 molecular transporter (5) was synthesized and used together with quantum dots in preparing the complexes (QD-MT). The QD-MT complexes were studied in terms of the cellular uptake and the internalization mechanism in live HeLa cells with the aid of various known endocytosis inhibitors. It has been concluded that the QD-MT complex is internalized largely by macropinocytosis. The mouse tissue distribution of the QD-MT complex by i.p. and i.v. routes showed some organ selectivity and a good ability to cross the BBB.