DI-87 is an orally active and selective deoxycytidine kinase (dCK) inhibitor with an EC 50 of 10.2 nM. DI-87 has antitumor activity and is used in combination therapy against tumors expressing dCK.
性状
Solid
IC50 & Target[1][2]
EC50: 10.2 nM (dCK)
体外研究(In Vitro)
(S)-DI-87 exhibits a much higher IC50 value (IC50=468 nM) relative to DI-87 ((R)-DI-8) (IC50=3.15 nM) in CEM T-ALL cells for inhibition of dCK activity. DI-87 (1 μM; for 72 hours) rescues human cell line CCRF-CEM (CEM) cells from the anti-proliferative effects of gemcitabine, a dCK-dependent nucleoside analog prodrug, with an EC50 of 10.2 nM. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
DI-87 (5-25 mg/kg; oral gavage) exhibits full dCK inhibition for 27 hours, and enzyme activity fully recovered by 36 hours with 25 mg/kg dose.
DI-87 (10-50 mg/kg; oral) has plasma concentrations of between 1 and 3 hours and plasma half-life of 4 hours.
DI-87 (10 mg/kg/day or 25 mg/kg/twice a day; oral; for 16-18 days) with thymidine (2 g/kg; ip; twice a day) results in reduced tumor growth in male NSG mice implanted with CEM tumors. 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]. Soumya Poddar, et al. Development and Preclinical Pharmacology of a Novel dCK Inhibitor, DI-87. Biochem Pharmacol. 2020 Feb;172:113742.
溶解度数据
In Vitro: DMSO : 100 mg/mL (198.95 mM; Need ultrasonic)配制储备液