AZ20

Catalog No.S7050

AZ20 Chemical Structure

Molecular Weight(MW): 412.51

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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3 Customer Reviews

  • (B) SAHA treatment impairs the HR capacity of GBM03 cells. AZ20(ATRi) as a positive control.

    Molecular Oncology, 2016, 1-13.. AZ20 purchased from Selleck.

    (c) AML cell lines and primary patient sample AML#53 were treated with AZ20 for 24 h and then subjected to annexin V-FITC/PI staining and flow cytometry analyses. Mean percent annexin V + cells ± SEM from one representative experiment performed in triplicates are shown. For cell lines, experiments were repeated three times, while patient sample experiments were performed once due to limited available sample.

    Sci Rep, 2017, 7:41950. AZ20 purchased from Selleck.

  • A. HeLa cells were first exposed for 1 hour to either no drug (black diamond) or a combination of 2 μM KU-60019 and 1 μM VE-821 (white circle) before addition of either trabectedin (left panel) or lurbinectedin (right panel) at the indicated concentrations. B. HeLa cells were first exposed for 1 hour to either no drug (black diamond) or a combination of 2 μM KU-60019 and 0.2 μM AZ20 (white circle) before addition of either trabectedin (left panel) or lurbinectedin (right panel) at the indicated concentrations. Both combinations of checkpoint abrogators, that is 2 μM KU-600019 with 1 μM VE-821 and 2 μM KU-600019 with 0.2 μM AZ20 have minor cytotoxic activity (

    Oncotarget, 2016, 7(18):25885-901. AZ20 purchased from Selleck.

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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.
Features ATR-selective inhibitor with high permeability and good stability.
Targets
ATR [2]
(Cell-free assay)
mTOR [2]
(Cell-free assay)
5 nM 38 nM
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HT29 cells M{TWZmZ2dmO2aX;uJIF{e2G7 Mon4NUBp NXLmRXZpyqCLbnjpZol1cW:wIH;mJGFVWi2vZXTpZZRm\CCFSFuxJJBpd3OyaH;yfYxifGmxbjDheEB{\XKrbnWgN|Q2KGmwIHj1cYFvKEiWMkmgZ4VtdHNiYX\0[ZIhOSCqcjDpckBxemW|ZX7j[UBw\iB2LX7peJJweXWrbn;sbY5mKDFvb4jp[IUtKEmFNUC9NE4xPSEQvF2= NXGwdmdTOjN|OUSyNFU>
LoVo cells MUnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkL2O|IhcA>? NUTJVVN1T3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hVG:YbzDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSVIHHzd4F6NCCJSUWwQVAvOiEQvF2= MmnhNlM{QTR{MEW=
human MDA-MB-468 cells NV;CPZljTnWwY4Tpc44h[XO|YYm= NWjqbYJmUW6qaXLpeIlwdiCxZjDtWG9TNW2nZHnheIVlKEGNVDDwbI9{eGixconsZZRqd25iYYSgd4VzcW6nIES3N{BqdiCqdX3hckBOTEFvTVKtOFY5KGOnbHzzMEBKSzVyPUKuOEDPxE1? Mof0NlM{QTR{MEW=

... Click to View More Cell Line Experimental Data

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]

Protocol

Animal Research:[2]
+ Expand
  • Animal Models: LoVo colorectal adenocarcinoma xenografts
  • Formulation: 10% DMSO/40% propylene glycol/50% water
  • Dosages: 25 mg/kg twice daily and 50 mg/kg once daily
  • Administration: orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 83 mg/mL (201.2 mM)
Ethanol 3 mg/mL (7.27 mM)
Water 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.

Chemical Information

Molecular Weight 412.51
Formula

C21H24N4O3S

CAS No. 1233339-22-4
Storage powder
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

  • Question 1:

    If I want to completely block the kinase activity from the in vitro cell lines, how much concentration I should use?

  • Answer:

    IC50 5nM was quoted from a previous publication in which the author tested IC50 of AZ20 in cell free assay. In cell culture, many factors, such as membrane permeability and target protein concentration, may affect the efficiency. Each cell line responses to the same compound differently and it is very difficult to predict the optimized concentration simply based on cell free data. In cell culture experiment, the required concentration is usually higher. We recommend that you perform a pilot experiment and test different concentrations (50nM to 500uM) to get the optimized condition.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID