AZ 20

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Cat.No. 5198 - AZ 20 | C21H24N4O3S | CAS No. 1233339-22-4
Description: Potent and selective ATR kinase inhibitor; antitumor
Chemical Name: 4-[4-[(3R)-3-Methyl-4-morpholinyl]-6-[1-(methylsulfonyl)cyclopropyl]-2-pyrimidinyl]-1H-indole
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature

Biological Activity

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.

Licensing Information

Sold for research purposes under agreement from AstraZeneca

Compound Libraries

AZ 20 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 412.51
Formula C21H24N4O3S
Storage Store at -20°C
Purity ≥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

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 20.63 50
ethanol 4.13 10

Preparing Stock Solutions

The following data is based on the product molecular weight 412.51. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.42 mL 12.12 mL 24.24 mL
5 mM 0.48 mL 2.42 mL 4.85 mL
10 mM 0.24 mL 1.21 mL 2.42 mL
50 mM 0.05 mL 0.24 mL 0.48 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

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


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View Related Products by Product Action

View all ATM and ATR Kinase Inhibitors

Keywords: AZ20 potent selective ATR Kinase inhibitors inhibits ataxia telangiectasia Rad3 related antitumor antitumour replication stress ATM & ATR Kinase

Citations for AZ 20

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Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
Cell Cycle & DNA Damage Repair

Cell Cycle & DNA Damage Repair Poster

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. Adapted from the 2015 Cancer Product Guide, Edition 3, 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.

Pathways for AZ 20

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