DI-82 is a potent deoxycytidine kinase (dCK) inhibitor with an IC₅₀^app of 27.8 nM and K_i^app of 9.2 nM. DI-82 has antitumor activity^[1].

IC50app: 27.8 nM (dCK)^[1]
Kiapp: 9.2 nM (dCK)^[1]

DI-82 (compound 12R) has an IC₅₀ of 3.7 nM in CCRF-CEM acute lymphoblastic leukemia cells^[1].
DI-82 (1 μM) has a NADPH-dependent CL_int of 22.7 μL/min•mg and a NADPH-dependent T_1/2 of 102 mins in a standard microsomal liver clearance assay^[1].
DI-82 (200 μM) completely blunts the ability of decitabine to bind human thymidylate synthase (TS)^[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

510.65

C₂₀H₂₆N₆O₄S₃

1638148-50-1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Julian Nomme, et al. Structure-guided Development of Deoxycytidine Kinase Inhibitors With Nanomolar Affinity and Improved Metabolic Stability. J Med Chem. 2014 Nov 26;57(22):9480-94.

  [2]. Helena Almqvist, et al. CETSA Screening Identifies Known and Novel Thymidylate Synthase Inhibitors and Slow Intracellular Activation of 5-fluorouracil. Nat Commun. 2016 Mar 24;7:11040.