Description
Ara-G is an analog of the nucleoside guanosine and an active metabolite of nelarabine . Ara-G accumulates in T lymphoblasts and malignant T-lymphoid cells, where it is phosphorylated to produce ara-GTP and incorporated into the DNA. Ara-G inhibits DNA replication by 92% after 30 minutes when used at a concentration of 50 μM in CEM cells, which are used as a model for human T lymphoblasts. It also halts the cell cycle at the sub-G
1 phase and induces apoptosis in CEM cells. Syngeneic bone marrow containing 6C3HED tumor cells treated with ara-G (100 mM)
ex vivo prior to transplantation increases survival of lethally irradiated mice and induces reconstitution of lymphoid, myeloid, and erythroid cell linages.
Uses
Ara-G is an inducer of apoptosis, inhibitor of DNA synthesis, an antimetabolite, and antineoplastic.
