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Purity: ≥98%
AZ32 is a novel, potent and orally bioavailable and blood-brain barrier-penetreable ATM inhibitor (AZ32) that radiosensitizes intracranial gliomas in mice. In an orthotopic mouse glioma model that is syngeneic and human, AZ32 demonstrated superior radiosensitization efficacy in vivo when compared to AZ31. In orthotopic mouse models, AZ32 is the first oral bioavailable ATMi that has been demonstrated to radiosensitize glioma and increase survival. These results lend credence to the creation of a clinical-grade, GBM-treating ATMi that penetrates the BBB. The use of an ATMi in conjunction with conventional radiotherapy is anticipated to be cancer-specific, boost the therapeutic ratio, and preserve the full therapeutic effect at lower radiation doses, which is significant because many GBMs have compromised p53 signalness.
| Targets |
ATM ( IC50 = 6.2 nM ); ATM ( IC50 = 0.31 μM )
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| Enzyme Assay |
AZ32 is a novel type of an ATM inhibitor that can penetrate the blood-brain barrier (BBB). GBM cells were radiosensitized in vitro by AZ32, which also inhibits the DNA damage response.
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| Cell Assay |
AZ32 (3 μM) and radiation (2 Gy) were applied to human glioma U1242-susceptible cells, or they were not treated. Anti-γ-tubulin (centrosomes) and -α-tubulin (microtubules) were used to fix and process the cells for ICC after 48 hours. To view nuclei, DAPI was used as a counterstain for the cells.
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| References |
| Molecular Formula |
C20H16N4O
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| Molecular Weight |
328.38
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| Exact Mass |
328.13
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| Elemental Analysis |
C, 73.15; H, 4.91; N, 17.06; O, 4.87
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| CAS # |
2288709-96-4
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| Appearance |
Solid powder
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| SMILES |
CNC(=O)C1=CC=C(C=C1)C2=CN=C3N2C=C(N=C3)C4=CC=CC=C4
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| InChi Key |
LCRTUEXVVKVKBD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H16N4O/c1-21-20(25)16-9-7-15(8-10-16)18-11-23-19-12-22-17(13-24(18)19)14-5-3-2-4-6-14/h2-13H,1H3,(H,21,25)
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| Chemical Name |
N-methyl-4-(6-phenylimidazo[1,2-a]pyrazin-3-yl)benzamide
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.61 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.61 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.61 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0453 mL | 15.2263 mL | 30.4525 mL | |
| 5 mM | 0.6091 mL | 3.0453 mL | 6.0905 mL | |
| 10 mM | 0.3045 mL | 1.5226 mL | 3.0453 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
 Radiosensitization of glioma cell lines by AZ32in vitro.Mol Cancer Ther.2018Aug;17(8):1637-1647. |
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 Radiosensitization of glioma by AZ32in vivo.Mol Cancer Ther.2018Aug;17(8):1637-1647. |
 Increased mitotic aberrations in glioma cells exposed to AZ32 and radiation.Mol Cancer Ther.2018Aug;17(8):1637-1647. |
 Combination of AZ32 and radiation induces mitotic catastrophe in mouse GL261 glioma cells.Mol Cancer Ther.2018Aug;17(8):1637-1647. |
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