AZ 20
Chemical Name: 4-[4-[(3R)-3-Methyl-4-morpholinyl]-6-[1-(methylsulfonyl)cyclopropyl]-2-pyrimidinyl]-1H-indole
Purity: ≥98%
Biological Activity
AZ 20 is a potent and selective ATR kinase inhibitor (IC50 = 5 nM). Exhibits 7.6-fold selectivity over mTOR and selectivity over a panel of 442 kinases, including ATM kinase, PI3-K isoforms, and DNA-PK. Inhibits cell growth in cell lines with high baseline levels of replication stress. Displays antitumor effects in vivo.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Additional Information
Background References
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Inhibiting checkpoint kinase 1 protects bone from bone resorption by mammary tumor in a mouse model
S Liu, Y Liu, K Minami, A Chen, Q Wan, Y Yin, L Gan, A Xu, N Matsuura, M Koizumi, Y Liu, S Na, J Li, H Nakshatri, BY Li, H Yokota
Oncotarget, 2018;9(10):9364-9378. -
Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity.
Foote et al.
J.Med.Chem., 2013;56:2125
Product Datasheets
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Citations for AZ 20
The citations listed below are publications that use Tocris products. Selected citations for AZ 20 include:
8 Citations: Showing 1 - 8
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Etoposide-induced DNA damage is increased in p53 mutants: identification of ATR and other genes that influence effects of p53 mutations on Top2-induced cytotoxicity.
Authors: Daniel Et al.
Oncotarget 2022;13:332-346
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MYBL2 and ATM suppress replication stress in pluripotent stem cells.
Authors: George Et al.
EMBO Rep 2021;22:e51120
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ATR is essential for preservation of cell mechanics and nuclear integrity during interstitial migration.
Authors: Jiri Et al.
Nat Commun 2020;11:4828
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Phase separation of 53BP1 determines liquid-like behavior of DNA repair compartments.
Authors: Kilic Et al.
EMBO J 2019;:e101379
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Efficient Pre-mRNA Cleavage Prevents Replication-Stress-Associated Genome Instability.
Authors: Teloni Et al.
Mol Cell 2019;73:670
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A Compendium of Mutational Signatures of Environmental Agents.
Authors: Stephen P Et al.
Cell 2019;177:821-836.e16
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BET Inhibition Induces HEXIM1- and RAD51-Dependent Conflicts between Transcription and Replication.
Authors: Bowry Et al.
Cell Rep 2018;25:2061
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FMN2 Makes Perinuclear Actin to Protect Nuclei during Confined Migration and Promote Metastasis.
Authors: Skau Et al.
Cell 2016;167:1571
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