NUC-7738, an aryloxy phosphoramidate of 3′-Deoxyadenosine, is a 5′-aryloxy phosphoramidate prodrug of 3′-Deoxyadenosine (3′-dA). NUC-7738 has potent cytotoxic activity against a panel of hematological cancer cell lines. NUC-7738 can be used in research of cancer.In Vitro:NUC-7738 (compound 7a; 0-198 μM; 72 h; CCRF-CEM, HL-60, KG-1, MOLT-4, K562, MV4-11, THP-1, HEL92, NCI-H929, RPMI-8226, Jurkat, Z138, RL, HS445, HepG2, MCF-7, Bx-PC-3, HT29, MIA PaCa-2 and SW620 cells) has anticancer activity and cytotoxic activity against a lineage of leukocytes with LC50 values of ＜30 μM.
NUC-7738 (1 μM) has good stability in human hepatocytes with t1/2 value of 48.1 min.
NUC-7738 has increased stability in human plasma compared to the parent nucleoside, with no change in plasma concentration up to 4 h.