Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DNA-PK-IN-8(化合物DK1)是一种高效、选择性且口服活性的DNA依赖蛋白激酶 (DNA-PK) 抑制剂,其IC50值为0.8 nM。与Doxorubicin联合应用时,该化合物能在多种癌细胞中展现出协同的抗增殖效应,并能显著地抑制HL-60肿瘤生长。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 10,600 | 10-14周 | ||
50 mg | ¥ 13,800 | 10-14周 | ||
100 mg | ¥ 17,500 | 10-14周 |
产品描述 | DNA-PK-IN-8 is a potent, selective, and orally active inhibitor of DNA-dependent protein kinase (DNA-PK), demonstrating an IC50 value of 0.8 nM. It displays synergistic antiproliferative effects across various cancer cell lines and notably reduces HL-60 tumor growth when combined with Doxorubicin [1]. |
体外活性 | DNA-PK-IN-8 (compound DK1) decreases the expression levels of γH2A.X in a concentration-dependent manner in HCT-116 cells [1]. Immunofluorescence Cell Line: HCT-116 (treated with Bleomycin for 6 hours) [1] Concentration: 1, 5, and 10 μM Incubation Time: 6 hours Result: Decreased the expression levels of γH2A.X in a concentration-dependent manner. |
体内活性 | DNA-PK-IN-8 (100 mg/kg; PO; QD for 16 days) significantly suppresses HL-60 tumor growth when co-administrating with Doxorubicin [1]. DNA-PK-IN-8 (5 mg/kg; PO; single dosage) exhibits reasonable pharmacokinetic properties in vitro and in vivo as an oral drug candidate [1]. Pharmacokinetic Parameters of DNA-PK-IN-8 in Sprague-Dawley rats [1]. PO (5 mg/kg) T max (h) 0.42 ± 0.11 t 1/2 (h) 1.59 ± 0.26 C max (ng/mL) 810 ± 122.32 AUC 0-∞ (ng/mL·h) 3598.7 ± 769.81 MRT 0-∞ (h) 2.29 ± 0.18 Animal Model: HL-60 tumor-bearing nude mice model [1] Dosage: 100 mg/kg Administration: PO; QD for 16 days Result: Led to significant tumor-suppressing effects with TGI values of 52.4% and 62.4% for tumor weight and tumor volume, respectively, when co-administrated with Doxorubicin. Animal Model: Sprague-Dawley rats [1] Dosage: 5 mg/kg Administration: PO; single dosage (Pharmacokinetic Analysis) Result: Exhibited reasonable pharmacokinetic properties in vitro and in vivo as an oral drug candidate. |
分子量 | 394.43 |
分子式 | C19H22N8O2 |
CAS No. | 2823369-81-7 |
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。
DNA-PK-IN-8 2823369-81-7 Inhibitor inhibitor inhibit