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Technical Data
| Formula | C21H24N4O3S |
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| Molecular Weight | 412.51 | CAS No. | 1233339-22-4 | |
| Solubility (25°C)* | In vitro | DMSO | 83 mg/mL (201.2 mM) | |
| Ethanol | 4 mg/mL (9.69 mM) | |||
| Water | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Biological Activity
| Description | AZ20 is a novel potent and selective inhibitor of ATR kinase with IC50 of 5 nM in a cell-free assay, 8-fold selectivity over mTOR. | ||||
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| In vitro | AZ20 shows good selectivity against all of the PI3K isoforms together with ATM and DNA-PK. [2] In vitro, AZ20 decreases pChk1 Ser345, pChk1 Ser317 and pChk1 Ser296 levels in a concentration-dependent manner. Prolonged exposure with AZ20 increases γH2AX pan-nuclear staining, indicative of replication stress. This is associated with S-phase arrest and increase in phospho-histone H3. AZ20 induces growth inhibition and cell death in vitro and its profile of activity is distinct from other cytotoxic agents. The cytotoxic effect of AZ20 can be increased in combination with the selective ATM inhibitor KU-60019. [1] | ||||
| In vivo | Female nude mice bearing LoVo tumors are treated with AZ20 orally at a dose of 25 mg/kg twice daily or 50 mg/kg once daily for 13 days, led to significant tumor growth inhibition. [2] This is associated with a persistent elevation of γH2AX pan-nuclear staining in xenograft tissue, but a transient increase in mouse bone marrow at therapeutic doses, suggesting a favourable therapeutic index. [1] AZ20 is assessed for drug−drug interaction (DDI) potential specifically from inhibition of cytochrome P450 enzymes. AZ20 is found to inhibit the cytochrome 3A4-mediated metabolism of midazolam by 50% at 10 μM. AZ20 has respectable bioavailability in a low dose rat PK study. [2] | ||||
| Features | ATR-selective inhibitor with high permeability and good stability. |
Protocol (from reference)
| Animal Study:[2] |
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References
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Customer Product Validation
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Data from [Data independently produced by , , Molecular Oncology, 2016, 1-13.]
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Data from [Data independently produced by , , Sci Rep, 2017, 7:41950]
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Data from [Data independently produced by , , Oncotarget, 2016, 7(18):25885-901]
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Data from [Data independently produced by , , Oncol Rep, 2018, 37(6):3377-3386]
Selleck's AZ20 has been cited by 49 publications
| The GATAD2B-NuRD complex drives DNA:RNA hybrid-dependent chromatin boundary formation upon DNA damage [ EMBO J, 2024, 10.1038/s44318-024-00111-7] | PubMed: 38719994 |
| Replicative senescence is ATM driven, reversible, and accelerated by hyperactivation of ATM at normoxia [ bioRxiv, 2024, 2024.06.24.600514] | PubMed: 38979390 |
| OTUD5 limits replication fork instability by organizing chromatin remodelers [ Nucleic Acids Res, 2023, 51(19):10467-10483] | PubMed: 37713620 |
| Actionable cancer vulnerability due to translational arrest, p53 aggregation and ribosome biogenesis stress evoked by the disulfiram metabolite CuET [ Cell Death Differ, 2023, 10.1038/s41418-023-01167-4] | PubMed: 37142656 |
| OTUD5 limits replication fork instability by organizing chromatin remodelers [ Nucleic Acids Res, 2023, gkad732] | PubMed: 37713620 |
| ATR protects ongoing and newly assembled DNA replication forks through distinct mechanisms [ Cell Rep, 2023, 42(7):112792] | PubMed: 37454295 |
| Adeno-Associated Virus Monoinfection Induces a DNA Damage Response and DNA Repair That Contributes to Viral DNA Replication [ mBio, 2023, e0352822.] | PubMed: 36719192 |
| Inhibition of DNA-dependent protein kinase catalytic subunit boosts rAAV transduction of polarized human airway epithelium [ Mol Ther Methods Clin Dev, 2023, 31:101115] | PubMed: 37841417 |
| Involvement of ATR-CHK1 pathway in fish megalocytivirus infection induced DNA-damage response in vitro [ Aquaculture, 2023, Volume 575] | PubMed: none |
| ATR activation by Cr-DNA damage is a major survival response establishing late S and G2 checkpoints after Cr-VI) exposure [ Toxicol Appl Pharmacol, 2023, 477:116696] | PubMed: 37734571 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.