AZ20

Catalog No.S7050

For research use only.

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.

AZ20 Chemical Structure

CAS No. 1233339-22-4

Selleck's AZ20 has been cited by 35 publications

Purity & Quality Control

Choose Selective ATM/ATR Inhibitors

Other ATM/ATR Products

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 NH;rRlBHfW6ldHnvckBie3OjeR?= M1vMXlEhcHJ? MV\Jcohq[mm2aX;uJI9nKEGWUj3t[YRq[XSnZDDDTGsyKHCqb4PwbI9zgWyjdHnvckBifCC|ZYLpcoUhOzR3IHnuJIh2dWGwIFjUNlkh[2WubIOgZYZ1\XJiMTDodkBqdiCycnXz[Y5k\SCxZjC0MY5qfHKxcYXpco9tcW6nIEGtc5hq\GVuIFnDOVA:OC5yNd88US=> M1zEclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{m0NlA2Lz5{M{O5OFIxPTxxYU6=
LoVo MoDYS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MW[3NkBpenN? NHP6doJIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBNd1[xIHPlcIx{KGGodHXyJFczKGi{czDifUBOXFNiYYPzZZktKEeLNUC9NE4z|ryP NYH4[mtKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzPVQzODVpPkKzN|k1OjB3PD;hQi=>
MDA-MB-468 M1vGPWZ2dmO2aX;uJIF{e2G7 MmW3TY5pcWKrdHnvckBw\iCvVF;SMY1m\GmjdHXkJGFMXCCyaH;zdIhwenmuYYTpc44h[XRic3XybY5mKDR5MzDpckBpfW2jbjDNSGEuVUJvNE[4JINmdGy|LDDJR|UxRTJwNN88US=> M1nCb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{m0NlA2Lz5{M{O5OFIxPTxxYU6=
LoVo NFrSV2RCdnSrdIXtc5Ih[XO|YYm= M3jRcFUxKG2pL3vn NF3obmoyOyCmYYnz M1vmS2FvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFzvWo8h[2WubIOgfIVvd2e{YX\0[YQhcW5iU4fpd5MhdnVxboWgcY92e2ViYYPz[ZN{\WRiYYOgeJVud3JiZ4Lve5RpKGmwaHnibZRqd25iYYSgOVAhdWdxa3esJJBwKHGmIH\vdkAyOyCmYYnzJJJmdGG2aY\lJJRwKGOxboTyc4w> MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN7NEKwOUc,OjN|OUSyNFU9N2F-
LoVo Mnf3RY51cXS3bX;yJIF{e2G7 M{S2OFI2KG2pL3vn MoHjNVMh\GG7cx?= MYDBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCOb2\vJINmdGy|IIjlco9oemGodHXkJIlvKFO5aYPzJI52N263IH3veZNmKGG|c3Xzd4VlKGG|IIT1cY9zKGe{b4f0bEBqdmirYnn0bY9vKGG2IEK1JI1oN2upLDDwc{BjcWRiZn;yJFE{KGSjeYOgdoVt[XSrdnWgeI8h[2:wdILvcC=> NFLlUlI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O5OFIxPSd-MkOzPVQzODV:L3G+
HT29 NXXW[JVLTnWwY4Tpc44h[XO|YYm= NYrzOIFqPjBibXnudy=> MXnJcohq[mm2aX;uJI9nKEGWUjDpckBpfW2jbjDIWFI6KGOnbHzzJIFnfGW{IE[wJI1qdnNiYomgTI9m[2i|dDCzN|I2QCC|dHHpcolv\y2kYYPl[EBie3OjeTygTWM2OD1yLkC2Ne69VQ>? MnLZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB|NE[3O|IoRjNyM{S2O|czRC:jPh?=
LoVo MVvDfZRwfG:6aXPpeJkh[XO|YYm= MkfmO|IhcHK| M{DjPGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGxwXm9iY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VWyCjc4PhfUwhT0l3ME2wMlLPxE1? MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODN2Nke3Nkc,OzB|NE[3O|I9N2F-
MDA-MB-468 NUnzSYprTnWwY4Tpc44h[XO|YYm= MojyTY5pcWKrdHnvckBw\iCvVF;SJIlvKGi3bXHuJG1FSS2PQj20Olgh[2WubIOgZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5iN{DTOmshWzJ|NT:yN|YheGixc4Doc5J6dGG2aX;uMEBKSzVyPUCuO|LPxE1? MmnmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB|NE[3O|IoRjNyM{S2O|czRC:jPh?=
HT-29 NFe4VFlEgXSxdH;4bYNqfHliYYPzZZk> NH7OSnM4OiCqcoO= NEHTe4lEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJXC1{OTDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSVIHHzd4F6NCCJSUWwQVAvQTgQvF2= NHy2dZY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEO0Olc4Oid-M{CzOFY4PzJ:L3G+
LoVo MkfvSpVv[3Srb36gZZN{[Xl? M1nYcVI2KG2pL3vn NUe0U3pqQCCqcoO= MXrQcIF{dWFiY3;uZ4VvfHKjdHnvckBqdiCVd3nzd{BvfS:wdTDtc5V{\SC6ZX7v[5Ji\nSnZDD3bZRpKGi3bXHuJGxwXm9iY3XscJMh[XRiMkWgcYcwc2duIIDvJIJq\CCjZoTldkA5KGi{czygR5A:OS56zszN NXzUfm9ZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CzOFY4PzJpPkOwN|Q3Pzd{PD;hQi=>
MDA-MB-468 NFrDXG5HfW6ldHnvckBie3OjeR?= MWHJcohq[mm2aX;uJI9nKG2WT2KgbY4hcHWvYX6gUWRCNU2ELUS2PEBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiCDS2SgdIhwe3Cqb4L5cIF1cW:wIHH0JHM1PzNicnXzbYR2\SxiSVO1NF0zNjUQvF2= MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODN2Nke3Nkc,OzB|NE[3O|I9N2F-
LoVo MnniSpVv[3Srb36gZZN{[Xl? NXPybGFVPTBibXevb4c> NH63NG05KGi{cx?= NFOyXnNRdGG|bXGgZ49v[2WwdILheIlwdiCrbjDTe4l{eyCwdT;ueUBud3W|ZTD4[Y5w\3KjZoTl[EB4cXSqIHj1cYFvKEyxVn:gZ4VtdHNiYYSgOVAhdWdxa3esJJBwKHGmIHHmeIVzKDhiaILzMEBEeD1|LkZOwG0> Mof0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB|NE[3O|IoRjNyM{S2O|czRC:jPh?=
Assay
Methods Test Index PMID
Growth inhibition assay IC50 28176818
Western blot p-CDK1 / CDK1 / p-CDK2 / CDK2 ; γH2AX / RRM1 / RRM2 28176818
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 (from reference)

Animal Research:[2]
  • Animal Models: LoVo colorectal adenocarcinoma xenografts
  • Dosages: 25 mg/kg twice daily and 50 mg/kg once daily
  • Administration: orally

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 412.51
Formula

C21H24N4O3S

CAS No. 1233339-22-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1COCCN1C2=NC(=NC(=C2)C3(CC3)S(=O)(=O)C)C4=C5C=CNC5=CC=C4

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.

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.

Tags: buy AZ20 | AZ20 supplier | purchase AZ20 | AZ20 cost | AZ20 manufacturer | order AZ20 | AZ20 distributor