2. Cell Cycle/DNA Damage PI3K/Akt/mTOR Apoptosis
  3. DNA-PK ATM/ATR PI3K Apoptosis
  4. AZD-7648

AZD-7648 is a potent, orally active, selective DNA-PK inhibitor with an IC50 of 0.6 nM. AZD-7648 induces apoptosis and shows antitumor activity.

For research use only. We do not sell to patients.

AZD-7648 Chemical Structure

AZD-7648 Chemical Structure

CAS No. : 2230820-11-6

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Customer Review

Based on 13 publication(s) in Google Scholar

AZD-7648 Related Antibodies

Top Publications Citing Use of Products

View All ATM/ATR Isoform Specific Products:

View All Isoforms
ATM ATR

View All PI3K Isoform Specific Products:

View All Isoforms
PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

AZD-7648 is a potent, orally active, selective DNA-PK inhibitor with an IC50 of 0.6 nM. AZD-7648 induces apoptosis and shows antitumor activity[1].

IC50 & Target

DNA-PKcs

91.3 nM (IC50)

PI3Kγ

1.37 μM (IC50)

ATM

17.93 μM (IC50)

In Vitro

AZD7648 (0-30 μM) is a potent radiosensitizer[1].
AZD7648 (3 μM) increases sensitivity to doxorubicin[1].
AZD7648 (0.6 μM) enhances the activity of PARP inhibitor olaparib[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

AZD-7648 Related Antibodies

Western Blot Analysis[1]

Cell Line: IR (ionizing radiation)-treated A549 cells or OAW42 cells treated with doxorubicin
Concentration: 0.03, 0.1, 0.3, 1, 3, 10 and 30 μM for A549; 3 μM for OAW42
Incubation Time: 1 h for A549; 0.5, 2, 4, 8 and 16 h for OAW42
Result: Potently inhibited DNA-PKcs autophosphorylation at Ser2056. Downregulated pDNA-PKcs Ser2056, γH2AX Ser139 and pRPA32 Ser4/Ser8 phosphorylation at early time points (at 30 min, 2 h and 4 h). Resulted in increased levels of γH2AX and the apoptosis marker cleaved PARP1 compared with doxorubicin treatment alone at later time points (8 and 16 h).

Cell Cycle Analysis[1]

Cell Line: IR (ionizing radiation)-treated A549 cells or A549 cells
Concentration: 0-30 μM
Incubation Time: 48 h
Result: Arrested cell cycle at G2/M phase.
In Vivo

AZD-7648 (100 mg/kg; p.o.; once daily for 5 days) induces tumour growth inhibition and tumour regression[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Nude mice, A549 xenografts and NCI-H1299 xenografts[1]
Dosage: 100 mg/kg
Administration: Oral administration, once daily for 5 days
Result: Induced tumour growth inhibition in combination with IR in A549 xenografts and induced tumour regression in combination with IR in NCI-H1299 xenografts.
Clinical Trial
Molecular Weight

380.40

Formula

C18H20N8O2
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

CC1=CC2=NC=NN2C=C1NC3=NC=C(N(C)C(N4C5CCOCC5)=O)C4=N3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 8.33 mg/mL (21.90 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6288 mL 13.1441 mL 26.2881 mL
5 mM 0.5258 mL 2.6288 mL 5.2576 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  0.5% HPMC  0.1%Tween80

    Solubility: 10 mg/mL (26.29 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.86%

COA (251 KB) HNMR (263 KB) LCMS (264 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6288 mL 13.1441 mL 26.2881 mL 65.7203 mL
5 mM 0.5258 mL 2.6288 mL 5.2576 mL 13.1441 mL
10 mM 0.2629 mL 1.3144 mL 2.6288 mL 6.5720 mL
15 mM 0.1753 mL 0.8763 mL 1.7525 mL 4.3814 mL
20 mM 0.1314 mL 0.6572 mL 1.3144 mL 3.2860 mL
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AZD-7648 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AZD-76482230820-11-6AZD7648AZD 7648DNA-PKATM/ATRPI3KApoptosisDNA-dependent protein kinaseAtaxia telangiectasia mutatedATM and RAD3 relatedPhosphoinositide 3-kinaseA549OAW42antitumorInhibitorinhibitorinhibit

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