DNA-PK-IN-8

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

DNA-PK-IN-8 

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。

DNA-PK-IN-8

DNA-PK-IN-8 Chemical Structure

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生物活性

DNA-PK-IN-8 is a highly potent, selective and orally active DNA-dependent protein kinase (DNA-PK) inhibitor with an IC50 value of 0.8 nM. DNA-PK-IN-8 exhibits synergistic antiproliferative activity against a series of cancer cell lines and significantly suppresses HL-60 tumor growth, when using in combination with Doxorubicin[1].

IC50 & Target

IC50: 0.8 nM (DNA-PK)[1]
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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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

Formula

C19H22N8O2
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]. Ding Z, et al. Discovery of novel 7,8-dihydropteridine-6(5H)-one-based DNA-PK inhibitors as potential anticancer agents via scaffold hopping strategy. Eur J Med Chem. 2022;237:114401.

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