Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DI-87 is a potent, orally active deoxycytidine kinase (dCK) inhibitor with high selectivity and an EC 50 of 10.2 nM. With demonstrated antitumor efficacy, DI-87 is employed in combination therapy specifically targeting tumors that express dCK.
产品描述 | DI-87 is a potent, orally active deoxycytidine kinase (dCK) inhibitor with high selectivity and an EC 50 of 10.2 nM. With demonstrated antitumor efficacy, DI-87 is employed in combination therapy specifically targeting tumors that express dCK. |
靶点活性 | DCK:10.2 nM (EC50) |
体外活性 | (S)-DI-87 exhibits a much higher IC 50 value (IC 50 =468 nM) relative to DI-87 ((R)-DI-8) (IC 50 =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 EC 50 of 10.2 nM[1]. |
体内活性 | 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]. 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 |
分子式 | C23H30N6O3S2 |
CAS No. | 2107280-55-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
DI-87 2107280-55-5 DI 87 DI87 Inhibitor inhibitor inhibit