FTY720 can be phosphorylated by sphingosine kinase, which then acts as a potent agonist at four of the sphingosine-1-phosphate (S1P) receptors (S1P1, S1P3, S1P4, and S1P5). IC₅₀ of (S)- and (R)- FTY720-phosphate on lymphocyte migration toward 10 nM of S1P are 0.137 nM and 10.98 nM respectively. The IC₅₀ values to cell lines MCF-7 is 6.8±0.6 µM.