DI-82 is a potent deoxycytidine kinase (dCK) inhibitor with an IC 50 of 27.8 nM and K i of 9.2 nM. DI-82 has antitumor activity.
性状
Solid
IC50 & Target[1][2]
IC50app: 27.8 nM (dCK)
Kiapp: 9.2 nM (dCK)
体外研究(In Vitro)
DI-82 (compound 12R) has an IC50 of 3.7 nM in CCRF-CEM acute lymphoblastic leukemia cells. 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. DI-82 (200?μM) completely blunts the ability of decitabine to bind human thymidylate synthase (TS). has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[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.
溶解度数据
In Vitro: DMSO : 100 mg/mL (195.83 mM; ultrasonic and warming and heat to 60°C)配制储备液