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Superparamagnetic FePt nanoparticles (NPs) have attracted considerable attention due to their extremely promising potentials as the diagnostic and therapeutic reagent in biomedical fields.In the present study, we developed a facile route to synthesize water-soluble FePtNPsabout 4 nm in diameter and oil-soluble FePtNPs about 6 nm in diameter using amino acids and oleic acid/oleylamine as the capping reagent, respectively.The component, size and magnetic property of FePt NPs were tuned through adjusting the reactant molar ratio.Furthermore, the anticancer activities of FePt NPs were evaluated using different brain tumor cell lines (such as U251, U87, H4) as the model.The growth prohibition of tumor cells by NPs was measured through MTT assay, while the interaction of NPs and tumor cells was observed through transmission electron microscopy (TEM).The results show that FePt NPs synthesize by oleic acid/oleylamine shows better cytotoxicity toward brain tumor cells than L-cysteine-synthesized FePt NPs.Obvious cellular uptake, intracellular trafficking, and uptake pathways of FePt NRs in three cells were similar.In conclusion,we developed a facile synthesis of water-soluble superparamagnetic FePt NPs with the different component and the different anticancer activity of FePt NPs on Human brain tumor cells were evaluated.These results provide a promising potential of superparamagnetic FePt NPs as the multifunctional diagnostic and therapeutic reagent in biomedical fields.