产品
编 号：F715071
分子式：C23H30N6O3S2
分子量：502.65
分子式：C23H30N6O3S2
分子量：502.65
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 2107280-55-5
产品详情
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.
体内研究：
DI-87 (5-25 mg/kg；口服强饲法) 在 27 小时内表现出完全的 dCK 抑制，并且酶活性在 25 mg/kg 剂量下完全恢复 36 小时。 DI-87 (10-50 mg/kg；口服) 的血浆浓度为 1 至 3 小时，血浆半衰期为 4 小时。 DI-87 (10 mg/kg/天或 25 mg/kg/每天两次；口服；持续 16-18 天) 与胸苷 (2 g/kg；腹腔注射；每天两次) 一起使用可减少肿瘤植入 CEM 肿瘤的雄性 NSG 小鼠的生长。Animal Model:8-12 week-old male or female NSG mice with CEM tumor xenografts
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
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.
体外研究：
(S)- DI-87 表现出比 DI-87 ((R)-DI-8) 更高的 IC50 值 (IC50=468 nM) (IC50=3.15 nM) 在 CEM T-ALL 细胞中抑制 dCK 活性。 DI-87 (1 μM；持续 72 小时) 从吉西他滨的抗增殖作用中拯救人类细胞系 CCRF-CEM (CEM) 细胞，吉西他滨是一种 dCK 依赖性核苷类似物前药，EC50为 10.2 nM。
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.
体内研究：
DI-87 (5-25 mg/kg；口服强饲法) 在 27 小时内表现出完全的 dCK 抑制，并且酶活性在 25 mg/kg 剂量下完全恢复 36 小时。 DI-87 (10-50 mg/kg；口服) 的血浆浓度为 1 至 3 小时，血浆半衰期为 4 小时。 DI-87 (10 mg/kg/天或 25 mg/kg/每天两次；口服；持续 16-18 天) 与胸苷 (2 g/kg；腹腔注射；每天两次) 一起使用可减少肿瘤植入 CEM 肿瘤的雄性 NSG 小鼠的生长。Animal Model:8-12 week-old male or female NSG mice with CEM tumor xenografts
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
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.
体外研究：
(S)- DI-87 表现出比 DI-87 ((R)-DI-8) 更高的 IC50 值 (IC50=468 nM) (IC50=3.15 nM) 在 CEM T-ALL 细胞中抑制 dCK 活性。 DI-87 (1 μM；持续 72 小时) 从吉西他滨的抗增殖作用中拯救人类细胞系 CCRF-CEM (CEM) 细胞，吉西他滨是一种 dCK 依赖性核苷类似物前药，EC50为 10.2 nM。
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备