Shanghai Nianxing Industrial Co., Ltd
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Product Name: DI-82
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1638148-50-1

1638148-50-1 structure

1638148-50-1 structure

Name: DI-82
Chemical Name: DI-82
CAS Number: 1638148-50-1
Molecular Formula: C₂₀H₂₆N₆O₄S₃
Molecular Weight: 510.65
Catalog: Signaling Pathways Others Others
Create Date: 2020-08-10 20:59:14
Modify Date: 2024-01-08 19:15:46
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].

Name	DI-82

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.

Molecular Formula	C₂₀H₂₆N₆O₄S₃
Molecular Weight	510.65