DI-87 ((R)-DI-87, TRE-515) is a highly potent, specific, orally bioavailable deoxycytidine kinase (dCK) inhibitor with IC50 of 3.15 nM.
(R)-DI-87 treatment rescued CEM cells from the anti-proliferative effects of gemcitabine, a dCK-dependent nucleoside analog prodrug, with an EC50 of 10.2 nM.
(R)-DI-87 is a promising new compound for use in combination therapy against tumors expressing dCK.
