DI-87

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DI-87 

DI-87 是一种具有口服活性的，选择性的脱氧胞苷激酶 (dCK) 抑制剂，EC50 为 10.2 nM。DI-87 具有抗肿瘤活性，可通过联合用药来抑制表达 dCK 的肿瘤。

DI-87

DI-87 Chemical Structure

CAS No. : 2107280-55-5

规格 价格 是否有货
5 mg ￥8500 询问价格 & 货期
10 mg ￥14500 询问价格 & 货期

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生物活性

DI-87 is an orally active and selective deoxycytidine kinase (dCK) inhibitor with an EC50 of 10.2 nM. DI-87 has antitumor activity and is used in combination therapy against tumors expressing dCK[1].

IC50 & Target

EC50: 10.2 nM (dCK)[1]
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[1].
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[1].

上海金畔生物科技有限公司 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[1].
DI-87 (10-50 mg/kg; oral) has plasma concentrations of between 1 and 3 hours and plasma half-life of 4 hours[1].
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[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 8-12 week-old male or female NSG mice with CEM tumor xenografts[1]
Dosage: 5, 10, 25 mg/kg
Administration: Oral gavage
Result: The 25 mg/kg dose exhibited full dCK inhibition for 27 hours, and enzyme activity fully recovered by 36 hours. The 10 mg/kg dose resulted in full inhibition with recovery initiating at the 12 hours time point. The 5 mg/kg dose resulted in minimal dCK inhibition with rapid recovery.
Animal Model: Female NSG mice with CEM tumors[1]
Dosage: 10, 25, or 50 mg/kg
Administration: Oral
Result: Had plasma concentrations of between 1 and 3 hours and plasma half-life of 4 hours.
Had tumor concentrations lower than plasma and had a later, more sustained peak at 3-9 hours.

分子量

502.65

Formula

C23H30N6O3S2
CAS 号

2107280-55-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

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

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