Art. -Nr.: HY-119653

AZ9482

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AZ9482 is a triple PARP1/2/6 inhibitor, with IC₅₀ values of 1 nM, 1 nM and 640 nM for PARP1, PARP2 and PARP6, respectively.

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Reinheit: 99.80%
CAS. Nr.: 1825345-33-2
Formel: C₂₆H₂₂N₆O₂
Molecular Weight:450.49

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

AZ9482 Chemical Structure

CAS. Nr.: 1825345-33-2

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

AZ9482 is a triple PARP1/2/6 inhibitor, with IC₅₀ values of 1 nM, 1 nM and 640 nM for PARP1, PARP2 and PARP6, respectively^[1].

Alle PARP Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	EC₅₀	<0.018 μM Compound: 1; AZ9482	Inhibition of PARP in human HeLa cells assessed as induction of centrosome declustering after 48 hrs by DAPI-staining based image analysis Inhibition of PARP in human HeLa cells assessed as induction of centrosome declustering after 48 hrs by DAPI-staining based image analysis	[PMID: 26546219]
MCF7	EC₅₀	123 nM Compound: 1; AZ9482	Inhibition of PARP in multi-drug resistant human MCF7 cells assessed as induction of centrosome declustering after 48 hrs by DAPI-staining based image analysis Inhibition of PARP in multi-drug resistant human MCF7 cells assessed as induction of centrosome declustering after 48 hrs by DAPI-staining based image analysis	[PMID: 26546219]
MDA-MB-468	EC₅₀	3 nM Compound: 1; AZ9482	Inhibition of PARP in human MDA-MB-468 cells assessed as induction of centrosome declustering after 48 hrs by DAPI-staining based image analysis Inhibition of PARP in human MDA-MB-468 cells assessed as induction of centrosome declustering after 48 hrs by DAPI-staining based image analysis	[PMID: 26546219]
OCI-LY19	IC₅₀	0.003 μM Compound: 1; AZ9482	Cytotoxicity against human OCI-LY19 assessed as growth inhibition after 3 days by Alamar Blue assay Cytotoxicity against human OCI-LY19 assessed as growth inhibition after 3 days by Alamar Blue assay	[PMID: 26546219]
Sf9	IC₅₀	0.001 μM Compound: 1; AZ9482	Inhibition of full length human PARP1 expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay Inhibition of full length human PARP1 expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay	[PMID: 26546219]
Sf9	IC₅₀	0.001 μM Compound: 1; AZ9482	Inhibition of human PARP2 (2 to 583 residues) expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay Inhibition of human PARP2 (2 to 583 residues) expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay	[PMID: 26546219]
Sf9	IC₅₀	0.009 μM Compound: 1; AZ9482	Inhibition of human TNKS1 (1001 to 1327 residues) expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay Inhibition of human TNKS1 (1001 to 1327 residues) expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay	[PMID: 26546219]
Sf9	IC₅₀	0.16 μM Compound: 1; AZ9482	Inhibition of human TNKS2 (667 to 1166 residues) expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay Inhibition of human TNKS2 (667 to 1166 residues) expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay	[PMID: 26546219]
Sf9	IC₅₀	0.64 μM Compound: 1; AZ9482	Inhibition of full length human PARP6 expressed in a Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay Inhibition of full length human PARP6 expressed in a Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay	[PMID: 26546219]

In Vitro

AZ9482 exhibits an EC₅₀ of 24 nM in MDA-MB-468 cells^[1].
AZ0108 treatment prevents CHK1 MARylation and induces hyperphosphorylation of CHK1, contributing to MPS formation and dysregulation of the cell cycle^[1].

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

Cell Viability Assay^[1]

Cell Line:

MDA-MB-468 cells.
Concentration:

0-10 μM.
Incubation Time:

3 days.
Result:

EC₅₀ was 24 nM.

In Vivo

AZ0108 also displays toxicity in vivo, the molecular basis of which is currently undefined, limiting pharmacological evaluation of AZ0108^[1].

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

Chemical Information

CAS. Nr. 1825345-33-2
Appearance Solid
Molecular Weight 450.49
Formel C₂₆H₂₂N₆O₂
Color White to yellow
SMILES

O=C1NN=C(C2=CC=CC=C21)CC3=CC=CC(C(N4CCN(CC4)C5=NC=CC=C5C#N)=O)=C3
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 125 mg/mL (277.48 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2198 mL

11.0990 mL

22.1981 mL

5 mM

0.4440 mL

2.2198 mL

4.4396 mL

10 mM

0.2220 mL

1.1099 mL

2.2198 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
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: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: 2.08 mg/mL (4.62 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.08 mg/mL (4.62 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.62 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Ryan T Howard, et al. Structure-Guided Design and In-Cell Target Profiling of a Cell-Active Target Engagement Probe for PARP Inhibitors. ACS Chem Biol. 2020 Feb 21;15(2):325-333. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	2.2198 mL	11.0990 mL	22.1981 mL	55.4951 mL
	5 mM	0.4440 mL	2.2198 mL	4.4396 mL	11.0990 mL
	10 mM	0.2220 mL	1.1099 mL	2.2198 mL	5.5495 mL
	15 mM	0.1480 mL	0.7399 mL	1.4799 mL	3.6997 mL
	20 mM	0.1110 mL	0.5550 mL	1.1099 mL	2.7748 mL
	25 mM	0.0888 mL	0.4440 mL	0.8879 mL	2.2198 mL
	30 mM	0.0740 mL	0.3700 mL	0.7399 mL	1.8498 mL
	40 mM	0.0555 mL	0.2775 mL	0.5550 mL	1.3874 mL
	50 mM	0.0444 mL	0.2220 mL	0.4440 mL	1.1099 mL
	60 mM	0.0370 mL	0.1850 mL	0.3700 mL	0.9249 mL
	80 mM	0.0277 mL	0.1387 mL	0.2775 mL	0.6937 mL
	100 mM	0.0222 mL	0.1110 mL	0.2220 mL	0.5550 mL

Keywords

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AZ9482

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Heterocyclic Compound Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle PARP Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AZ9482

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Heterocyclic Compound Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle PARP Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AZ9482 Related Classifications

HY-119653 Related Classifications