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Submit ReviewAZ 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.
Sold for research purposes under agreement from AstraZeneca
AZ 20 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. 了解 Tocris 化合物库的更多信息。
分子量 | 412.51 |
公式 | C21H24N4O3S |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1233339-22-4 |
PubChem ID | 46244454 |
InChI Key | SCGCBAAYLFTIJU-CQSZACIVSA-N |
Smiles | CS(C4(CC4)C1=CC(N5[C@H](C)COCC5)=NC(C2=CC=CC3=C2C=CN3)=N1)(=O)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 20.63 | 50 | |
ethanol | 4.13 | 10 |
以下数据基于产品分子量 412.51。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.5 mM | 4.85 mL | 24.24 mL | 48.48 mL |
2.5 mM | 0.97 mL | 4.85 mL | 9.7 mL |
5 mM | 0.48 mL | 2.42 mL | 4.85 mL |
25 mM | 0.1 mL | 0.48 mL | 0.97 mL |
参考文献是支持产品生物活性的出版物。
Foote et al (2013) 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. J.Med.Chem. 56 2125 PMID: 23394205
If you know of a relevant reference for AZ 20, please let us know.
关键词: AZ 20, AZ 20 supplier, AZ20, potent, selective, ATR, Kinase, inhibitors, inhibits, ataxia, telangiectasia, Rad3, related, antitumor, antitumour, replication, stress, ATM, &, Checkpoint, Control, Kinases, 5198, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 AZ 20 的部分引用包括:
Teloni et al (2019) Efficient Pre-mRNA Cleavage Prevents Replication-Stress-Associated Genome Instability. Mol Cell 73 670 PMID: 30639241
Kilic et al (2019) Phase separation of 53BP1 determines liquid-like behavior of DNA repair compartments. EMBO J e101379 PMID: 31267591
George et al (2021) MYBL2 and ATM suppress replication stress in pluripotent stem cells. EMBO Rep 22 e51120 PMID: 33779025
Daniel et al (2022) 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. Oncotarget 13 332-346 PMID: 35178190
Stephen P et al (2019) A Compendium of Mutational Signatures of Environmental Agents. Cell 177 821-836.e16 PMID: 30982602
Bowry et al (2018) BET Inhibition Induces HEXIM1- and RAD51-Dependent Conflicts between Transcription and Replication. Cell Rep 25 2061 PMID: 30463005
Jiri et al (2020) ATR is essential for preservation of cell mechanics and nuclear integrity during interstitial migration. Nat Commun 11 4828 PMID: 32973141
Skau et al (2016) FMN2 Makes Perinuclear Actin to Protect Nuclei during Confined Migration and Promote Metastasis. Cell 167 1571 PMID: 27839864
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AZ20 (2.4 μM)
I used short treatments with AZ20 in the presence of JQ1.
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
This product guide provides a review of the cell cycle and DNA damage research area and lists over 150 products, including research tools for:
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. This poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.