Art. -Nr.: HY-112198

AZ31

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AZ31 is a a potent, highly selective, and orally active ATM inhibitor with an IC₅₀ of <1.2 nM for ATM enzyme, and an IC₅₀ of 46 nM for ATM in cell. AZ31 shows excellent selectivity over ATR (>500-fold) and excellent PIKK-family selectivity and pan-kinase selectivity. AZ31 is a potent radiosensitizer in vitro, it can be used for the research of cancer.

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Reinheit: 98.00%
CAS. Nr.: 2088113-98-6
Formel: C₂₄H₂₈N₄O₃
Molecular Weight:420.50

Speicherung:

-20°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

AZ31 Chemical Structure

CAS. Nr.: 2088113-98-6

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

ATM

1.2 nM (IC₅₀)

ATM

46 nM (IC₅₀, in cell)

Alle ATM/ATR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	>9 μM Compound: AZ31	Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 6 days by MTT assay Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 6 days by MTT assay	[PMID: 37438997]
HCT-116	IC₅₀	20.02 nM Compound: AZ31	Inhibition of colony formation in human HCT-116 cells preincubated for 1 hr followed by exposure to 2 Gy gamma irradiation and measured after 1 week by crystal violet staining based chemiluminescence assay Inhibition of colony formation in human HCT-116 cells preincubated for 1 hr followed by exposure to 2 Gy gamma irradiation and measured after 1 week by crystal violet staining based chemiluminescence assay	[PMID: 37438997]
HT-29	IC₅₀	>30 μM Compound: 72	Inhibition of ATR in human HT-29 cells assessed as reduction in Chk1 phosphorylation at Ser-345 residue after 60 mins in presence of 4-nitroquinoline-1-oxide by Hoechst 33258 staining based plate reader analysis Inhibition of ATR in human HT-29 cells assessed as reduction in Chk1 phosphorylation at Ser-345 residue after 60 mins in presence of 4-nitroquinoline-1-oxide by Hoechst 33258 staining based plate reader analysis	[PMID: 27259031]
HT-29	IC₅₀	>30 μM Compound: 72	Inhibition of DNAPK phosphorylation at Ser-2056 residue in human HT-29 cells Inhibition of DNAPK phosphorylation at Ser-2056 residue in human HT-29 cells	[PMID: 27259031]
HT-29	IC₅₀	0.046 μM Compound: 72	Inhibition of ATM phosphorylation at Ser-1981 residue in human HT-29 cells incubated for 1 hr followed by X-ray irradiation by Hoechst staining based fluorescence plate reader analysis Inhibition of ATM phosphorylation at Ser-1981 residue in human HT-29 cells incubated for 1 hr followed by X-ray irradiation by Hoechst staining based fluorescence plate reader analysis	[PMID: 27259031]
MCF7	IC₅₀	>9 μM Compound: AZ31	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 6 days by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 6 days by MTT assay	[PMID: 37438997]
MCF7	IC₅₀	0.09 μM Compound: AZ31	Synergistic antiproliferative activity against human MCF7 cells assessed as Etoposide IC50 at 200 nM measured after 6 days by MTT assay Synergistic antiproliferative activity against human MCF7 cells assessed as Etoposide IC50 at 200 nM measured after 6 days by MTT assay	[PMID: 37438997]
MCF7	IC₅₀	0.43 μM Compound: AZ31	Antiproliferative activity against human MCF7 cells assessed as irinotecan IC50 at 200 nM measured after 6 days by MTT assay Antiproliferative activity against human MCF7 cells assessed as irinotecan IC50 at 200 nM measured after 6 days by MTT assay	[PMID: 37438997]
SW-620	IC₅₀	>9 μM Compound: AZ31	Antiproliferative activity against human SW620 cells assessed as reduction in cell viability incubated for 6 days by MTT assay Antiproliferative activity against human SW620 cells assessed as reduction in cell viability incubated for 6 days by MTT assay	[PMID: 37438997]
SW-620	IC₅₀	0.07 μM Compound: AZ31	Synergistic inhibition of colony formation in human SW620 cells assessed as irinotecan IC50 at 200 nM preincubated for 1 hr followed by irinotecan addition and measured after 1 week by crystal violet staining based chemiluminescence assay Synergistic inhibition of colony formation in human SW620 cells assessed as irinotecan IC50 at 200 nM preincubated for 1 hr followed by irinotecan addition and measured after 1 week by crystal violet staining based chemiluminescence assay	[PMID: 37438997]
SW-620	IC₅₀	0.65 μM Compound: AZ31	Synergistic antiproliferative activity against human SW620 cells assessed as irinotecan IC50 at 200 nM measured after 6 days by MTT assay Synergistic antiproliferative activity against human SW620 cells assessed as irinotecan IC50 at 200 nM measured after 6 days by MTT assay	[PMID: 37438997]

In Vitro

AZ31 (0.3-3 μM; 1 h) affects phosphorylation of a panel of ATM targets^[1].
AZ31 (10 μM; 1 h) affects stabilization of p53 in H2228 lung cancer cells after radiation^[1].

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

Western Blot Analysis^[1]

Cell Line:

Human glioma cell line
Concentration:

0.3, 1 and 3 μM
Incubation Time:

1 hour
Result:

Blocked phosphorylation of p53-S15, KAP1-S824, and ATM auto-phosphorylation at S1981.

Western Blot Analysis^[1]

Cell Line:

H460 and mutant p53 H2228 cell lines
Concentration:

10 μM
Incubation Time:

1 hour
Result:

Destabilized p53 of mutant p53 but not wild-type after radiation.

In Vivo

AZ31 (50-100 mg/kg; p.o. twice a day) shows low brain coverage^[1].

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

Animal Model:

Nude mice^[1]
Dosage:

50 and 100 mg/kg
Administration:

Oral gavage; 50 and 100 mg/kg twice a day
Result:

Exhibited exposure over IC₅₀ at 0.046 μM in brain only for 2-3 hours.

Chemical Information

CAS. Nr. 2088113-98-6
Appearance Solid
Molecular Weight 420.50
Formel C₂₄H₂₈N₄O₃
Color Off-white to light yellow
SMILES

O=C(C1=C(N[C@@H](C)C2CCOCC2)C3=CC(C4=CC=C(COC)N=C4)=CC=C3N=C1)N
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (237.81 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

2.3781 mL

11.8906 mL

23.7812 mL

5 mM

0.4756 mL

2.3781 mL

4.7562 mL

10 mM

0.2378 mL

1.1891 mL

2.3781 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 (protect from light). 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)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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]. Karlin J, et al. Orally Bioavailable and Blood-Brain Barrier-Penetrating ATM Inhibitor (AZ32) Radiosensitizes Intracranial Gliomas in Mice. Mol Cancer Ther. 2018 Aug;17(8):1637-1647. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3781 mL	11.8906 mL	23.7812 mL	59.4530 mL
	5 mM	0.4756 mL	2.3781 mL	4.7562 mL	11.8906 mL
	10 mM	0.2378 mL	1.1891 mL	2.3781 mL	5.9453 mL
	15 mM	0.1585 mL	0.7927 mL	1.5854 mL	3.9635 mL
	20 mM	0.1189 mL	0.5945 mL	1.1891 mL	2.9727 mL
	25 mM	0.0951 mL	0.4756 mL	0.9512 mL	2.3781 mL
	30 mM	0.0793 mL	0.3964 mL	0.7927 mL	1.9818 mL
	40 mM	0.0595 mL	0.2973 mL	0.5945 mL	1.4863 mL
	50 mM	0.0476 mL	0.2378 mL	0.4756 mL	1.1891 mL
	60 mM	0.0396 mL	0.1982 mL	0.3964 mL	0.9909 mL
	80 mM	0.0297 mL	0.1486 mL	0.2973 mL	0.7432 mL
	100 mM	0.0238 mL	0.1189 mL	0.2378 mL	0.5945 mL

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AZ31

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Glucose Metabolism Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

Alle ATM/ATR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AZ31

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Glucose Metabolism Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

Alle ATM/ATR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AZ31 Related Classifications

HY-112198 Related Classifications