AZ31
Based on 1 Customer Validation
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.00%
- No. CAS: 2088113-98-6
- Fòrmula: C24H28N4O3
- Peso molecular:420.50
-
Almacenamiento:
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Pureza y Documentación
- Referencias
-
Help & FAQs
-
Cell Cycle/DNA Damage Compound Library
HY-L004
-
Kinase Inhibitor Library
HY-L009
-
PI3K/Akt/mTOR Compound Library
HY-L015
-
Anti-Cancer Compound Library
HY-L025
-
Anti-Aging Compound Library
HY-L034
-
Oxygen Sensing Compound Library
HY-L045
-
Glycolysis Compound Library
HY-L058
-
Cytoskeleton Compound Library
HY-L060
-
Anti-Lung Cancer Compound Library
HY-L075
-
Anti-Pancreatic Cancer Compound Library
HY-L077
-
Anti-Cancer Metabolism Compound Library
HY-L083
-
Anti-Obesity Compound Library
HY-L087
-
Glucose Metabolism Compound Library
HY-L092
-
Cancer Stem Cells Compound Library
HY-L135
-
Heterocyclic Compound Library
HY-L138
-
Highly Selective Inhibitors Library
HY-L158
-
Serine/Threonine Kinase Inhibitor Library
HY-L164
-
Anti-Ovarian Cancer Compound Library
HY-L173
-
Multi-Target Compound Library
HY-L176
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Bioactive Compound Library
HY-L001
-
Protein Kinase Compound Library
HY-L196
-
High-Throughput Bioactive Compound Library
HY-L205
-
Posttranslational Modification Library
HY-L226
-
High-Efficiency Gene Editing Compound Library
HY-L244
Actividad biológica
|
ATM 1.2 nM (IC50) |
ATM 46 nM (IC50, in cell) |
|
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] |
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.
-
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.
-
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.
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
-
No. CAS 2088113-98-6
-
Appearance Solid
-
Peso molecular 420.50
-
Fòrmula 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
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
-
Ficha de datos (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)
-
Instrucciones de manejo (2659 KB)
Referencias
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 (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.
| 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 |
AZ31 Related Classifications
HY-112198 Related Classifications
Powered by Bioz