To assess its suitability as a prodrug of 5-fluorouracil (5-FU), 1-glycyloxymethyl-5-FU HCl (GFU), a 5-fluorouracil derivative having a glycyloxymethyl group at the N-1 position was synthetized. Its physicochemical properties and hydrolysis kinetics, in aqueous solution of pH 1∼10 and in the presence of human plasma or rat liver homogenate were studied. Its acute toxicity and antitumor activity against sarcoma 180 were also examined. GFU showed higher lipid/water partition coefficient than 5-FU. The calculated pK_a values of 5-FU and GFU were 8.02 and 7.20, respectively. The decomposition rates of GFU in aqueous solution showed a pH-dependence over the pH range used, which could be ascribed to solvent catalysed hydrolysis reaction at pH lower than 4.16 and to specific hydroxide ion hydrolysis reaction at pH higher than 4.16. The half-life of GFU was 6.9 min in 80% human plasma solution and less than 3 min in rat liver homogenate at 37℃. The LD_(50) value of 5-FU was 240 ㎎/㎏ while that of GFU was 440.6 ㎎/㎏ (226 ㎎ as 5-FU). Both of 5-FU and GFU showed a strong antitumor activity. Therapeutic ratios of 5-FU and GFU were 3.07 and 3.55, respectively.