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DI-82

Names

[ CAS No. ]:
1638148-50-1

[ Name ]:
DI-82

Biological Activity

[Description]:

DI-82 is a potent deoxycytidine kinase (dCK) inhibitor with an IC50app of 27.8 nM and Kiapp of 9.2 nM. DI-82 has antitumor activity[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Others >> Others

[Target]

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


[In Vitro]

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 CLint of 22.7 μL/min•mg and a NADPH-dependent T1/2 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].

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C20H26N6O4S3

[ Molecular Weight ]:
510.65

Related Compounds