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Reagents and instruments for immunology, cell biology and molecular biology.

AZD-7648 [2230820-11-6]

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Cat# NB-64-39310-10mg

Size : 10mg

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Phone : +1 850 650 7790

Brand : Neo Biotech

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AZD-7648

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Synonyms:

Catalog No. T7122 Copy Product Info

Purity: 99.85%

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.

Cas No. 2230820-11-6

With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.85%

Appearance:Solid

Color:White

Product Information

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	DNA-PK:0.63 nM, PI3Kγ:1.37 μM, ATM:17.93 μM

Chemical Properties

Molecular Weight	380.4
Formula	C₁₈H₂₀N₈O₂
Cas No.	2230820-11-6
Smiles	Cc1cc2ncnn2cc1Nc1ncc2n(C)c(=O)n(C3CCOCC3)c2n1
Relative Density.	1.60 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Store 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

	1mg	5mg	10mg	50mg
1 mM	2.6288 mL	13.1441 mL	26.2881 mL	131.4406 mL
5 mM	0.5258 mL	2.6288 mL	5.2576 mL	26.2881 mL
10 mM	0.2629 mL	1.3144 mL	2.6288 mL	13.1441 mL
20 mM	0.1314 mL	0.6572 mL	1.3144 mL	6.5720 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

Calculator

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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:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 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 DMSO 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 DMSO stock solution to 400 µL PEG300 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 ddH₂O 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.

Dose Conversion

Keywords

PI3KPhosphoinositide 3-kinaseOAW42

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