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AZD-7648

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Catalog No. T7122Cas No. 2230820-11-6

AZD-7648 is an inhibitor of DNA-dependent protein kinase (DNA-PK) with the IC50 of 0.63 nM in an enzyme assay,has anti-tumor activity.

AZD-7648

AZD-7648

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Purity: 99.85%
Catalog No. T7122Cas No. 2230820-11-6
AZD-7648 is an inhibitor of DNA-dependent protein kinase (DNA-PK) with the IC50 of 0.63 nM in an enzyme assay,has anti-tumor activity.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$34In StockIn Stock
5 mg$80In StockIn Stock
10 mg$122In StockIn Stock
25 mg$197In StockIn Stock
50 mg$328In StockIn Stock
100 mg$497In StockIn Stock
200 mg$723In StockIn Stock
1 mL x 10 mM (in DMSO)$89In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.85%
Appearance:Solid
Color:White
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Product Introduction

AZD-7648 AI Summary
AZD-7648 exhibits potent bioactivity as a DNA-PK inhibitor, with an IC50 of 0.6-0.631 nM in TR-FRET assays involving the DNA-PK catalytic subunit in human HeLa cells. It also effectively inhibits DNA-PK in human A549 cells with an IC50 range of 91.0-100.0 nM, showing a selective preference over other kinases such as PI3K isoforms, ATM, ATR, and mTOR. The compound has favorable oral bioavailability in Han Wistar rats and Beagle dogs and demonstrates adequate solubility in simulated intestinal and gastric fluids. Additionally, it shows moderate to high plasma protein binding, and metabolic stability in human liver microsomes with an intrinsic clearance of 6.4 mL.min-1.g-1. AZD-7648 induces apoptosis in human HCT-116 cells, disrupts mitochondrial function, causes cell cycle arrest, and shows synergistic antiproliferative and antitumor activity in animal models. While demonstrating minimal effects on hERG expressed in CHO cells, the compound exhibits complex impacts on the thermal stability of various protein domains. Overall, AZD-7648's bioactivity and pharmacokinetic profiles suggest significant potential for further evaluation as a targeted DNA-PK inhibitor..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
AZD-7648 is an inhibitor of DNA-dependent protein kinase (DNA-PK) with the IC50 of 0.63 nM in an enzyme assay,has anti-tumor activity.
Targets&IC50
ATM:17.93 μM, PI3Kγ:1.37 μM, DNA-PK:0.63 nM
Chemical Properties
Molecular Weight380.4
FormulaC18H20N8O2
Cas No.2230820-11-6
SmilesCc1cc2ncnn2cc1Nc1ncc2n(C)c(=O)n(C3CCOCC3)c2n1
Relative Density.1.60 g/cm3 (Predicted)
Storage & Solubility Information
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 9.52 mg/mL (25.03 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.6288 mL13.1441 mL26.2881 mL131.4406 mL
5 mM0.5258 mL2.6288 mL5.2576 mL26.2881 mL
10 mM0.2629 mL1.3144 mL2.6288 mL13.1441 mL
20 mM0.1314 mL0.6572 mL1.3144 mL6.5720 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
% DMSO
%
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Tech Support

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

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