DNA-PK-IN-8 (compound DK1) 是一种高效且具有选择性和口服活性的DNA 依赖蛋白激酶 (DNA-PK)抑制剂，IC50为 0.8 nM。DNA-PK-IN-8 与 Doxorubicin 联合使用时，对一系列癌细胞具有协同抗增殖活性，并能显著抑制 HL-60 肿瘤的生长。
| 生物活性 | DNA-PK-IN-8 is a highly potent, selective and orally activeDNA-dependent protein kinase (DNA-PK)inhibitor with anIC50value of 0.8 nM. DNA-PK-IN-8 exhibits synergistic antiproliferative activity against a series ofcancercell lines and significantly suppresses HL-60 tumor growth, when using in combination with Doxorubicin[1]. |
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体外研究
(In Vitro) | 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. |
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体内研究
(In Vivo) | 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) | | Tmax(h) | 0.42 ± 0.11 | | t1/2(h) | 1.59 ± 0.26 | | Cmax(ng/mL) | 810 ± 122.32 | | AUC0-∞(ng/mL·h) | 3598.7 ± 769.81 | | MRT0-∞(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. |
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| 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. |
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