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DNA-PK-IN-8

Catalog No. T61828 CAS 2823369-81-7

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].

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DNA-PK-IN-8, CAS 2823369-81-7

Pack Size	Availability	Price/USD
25 mg	10-14 weeks	$ 1,520.00
50 mg	10-14 weeks	$ 1,980.00
100 mg	10-14 weeks	$ 2,500.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

Chemical Properties

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Description	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].
In vitro	DNA-PK-IN-8 (compound DK1) effectively reduces γH2A.X expression in a concentration-dependent manner in HCT-116 cells when administered at concentrations of 1, 5, and 10 μM for an incubation period of 6 hours, following pre-treatment with Bleomycin. This effect was confirmed through immunofluorescence analysis in the specified cell line [1].
In vivo	DNA-PK-IN-8, administered orally at a dose of 100 mg/kg daily for 16 days, significantly inhibited HL-60 tumor growth in nude mice when used in conjunction with Doxorubicin, demonstrating tumor growth inhibition (TGI) values of 52.4% and 62.4% for tumor weight and volume, respectively. Additionally, a single oral dose of DNA-PK-IN-8 at 5 mg/kg in Sprague-Dawley rats revealed favorable pharmacokinetic properties, both in vitro and in vivo, supporting its potential as an oral therapeutic candidate. The pharmacokinetic analysis in Sprague-Dawley rats showed a maximum plasma concentration (Cmax) of 810 ± 122.32 ng/mL, achieved at a median time (Tmax) of 0.42 ± 0.11 hours, with a half-life (t1/2) of 1.59 ± 0.26 hours and an area under the curve (AUC 0-∞) of 3598.7 ± 769.81 ng/mL·h, indicating its reasonable pharmacokinetic profile.

Molecular Weight	394.43
Formula	C19H22N8O2
CAS No.	2823369-81-7

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Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

DNA-PK-IN-8 2823369-81-7 inhibitor inhibit

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