VE-821

Catalog No.S8007

For research use only.

VE-821 is a potent and selective ATP competitive inhibitor of ATR with Ki/IC50 of 13 nM/26 nM in cell-free assays, shows inhibition of H2AX phosphorylation, minimal activity against PIKKs ATM, DNA-PK, mTOR and PI3Kγ.

VE-821 Chemical Structure

CAS No. 1232410-49-9

Selleck's VE-821 has been cited by 194 publications

Purity & Quality Control

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Biological Activity

Description VE-821 is a potent and selective ATP competitive inhibitor of ATR with Ki/IC50 of 13 nM/26 nM in cell-free assays, shows inhibition of H2AX phosphorylation, minimal activity against PIKKs ATM, DNA-PK, mTOR and PI3Kγ.
Targets
ATR [1]
(Cell-free assay)
13 nM(Ki)
In vitro

VE-821 shows excellent selectivity for ATR with minimal cross-reactivity against the related PIKKs ATM, DNA-PK, mTOR and PI3K (Kis of 16 μM, 2.2 μM, >1 μM and 3.9 μM, respectively. VE-821 alone commits a large fraction of cancer cell populations to death, but it only reversibly limits cell cycle progression in normal cells, with minimal death or long-term detrimental effects. VE-821 along with cisplatin treatment shows the most marked synergy. [1] VE-821 inhibits H2AX cell growth with IC50 of 800 nM. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
U2OS  M3TsbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHOTWM2OO,;nkCuPEDPxE1? NFzvdIs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUW5N|E5PCd-MkW1PVMyQDR:L3G+
SAOS2 MnfBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrmTWM2OO,;nkCuPEDPxE1? MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTV7M{G4OEc,OjV3OUOxPFQ9N2F-
CAL72 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|Ux973gMD64JO69VQ>? NX61SpU{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW1PVMyQDRpPkK1OVk{OTh2PD;hQi=>
NOS1 M1fIZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fRVmlEPTExv[6wMlgh|ryP NWfCU5VzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW1PVMyQDRpPkK1OVk{OTh2PD;hQi=>
HUO9 MmXQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|Ux973gMD64JO69VQ>? Ml\2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV3OUOxPFQoRjJ3NUmzNVg1RC:jPh?=
MG63 NEXPZpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mli0TWM2OO,;nkmg{txO Mn76QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV3OUOxPFQoRjJ3NUmzNVg1RC:jPh?=
SJSA1 MnvOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlGxTWM2OO,;nkmg{txO NWTtXXpZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW1PVMyQDRpPkK1OVk{OTh2PD;hQi=>
MDA-MB-231 Mly5R5l1d3SxeHnjbZR6KEG|c3H5 Ml3nNU8{NzFyIN88US=> NIPJ[2syKGh? NV\sbVBIeG:2ZX70bYF1\XNidHjlJIN6fG:2b4jpZ4l1gSCxZjDic5RpKGOjbYD0c5Rp\WOrbjDhcoQhVE2SLUSwNC=> MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ4OUS3PUc,OjV{Nkm0O|k9N2F-
HT-29 NGK0WlZEgXSxdH;4bYNqfHliQYPzZZk> M1rrdFEwOy9zMDFOwG0> NWC3bGlGOSCq MW\wc5RmdnSrYYTld{B1cGViY4n0c5RwgGmlaYT5JI9nKGKxdHigZ4FueHSxdHjlZ4lvKGGwZDDMUXAuPDBy NX\xVmVTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyOlk1PzlpPkK1NlY6PDd7PD;hQi=>
HCT-116 p53+/+ MoToR5l1d3SxeHnjbZR6KEG|c3H5 MnLONU8{NzFyIN88US=> M1m4RlEhcA>? MWnwc5RmdnSrYYTld{B1cGViY4n0c5RwgGmlaYT5JI9nKGKxdHigZ4FueHSxdHjlZ4lvKGGwZDDMUXAuPDBy MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ4OUS3PUc,OjV{Nkm0O|k9N2F-
HCT-116 p53-/- NXHhXGZCS3m2b4TvfIlkcXS7IFHzd4F6 NWXIPYdEOS9|L{GwJO69VQ>? NYP3[oVQOSCq NYfqUHhjeG:2ZX70bYF1\XNidHjlJIN6fG:2b4jpZ4l1gSCxZjDic5RpKGOjbYD0c5Rp\WOrbjDhcoQhVE2SLUSwNC=> M4e5XFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mk[5OFc6Lz5{NUK2PVQ4QTxxYU6=
TF-1 NIPaOXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPPb3dLOC5yMUJihLM5KM7:TR?= NWjjNXNvQTZiaB?= NEm0RlVmdmijbnPld{B1cGViYX70bZBzd2yrZnXyZZRqfmViZX\m[YN1eyCxZjDNT|E4PzV? MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDF5OUG1Nkc,OjRzN{mxOVI9N2F-
HEL MoXLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHRXWRXOC5yMUJihLM5KM7:TR?= NVvKPVhKQTZiaB?= Mlq1[Y5p[W6lZYOgeIhmKGGwdHnwdo9tcW[ncnH0bZZmKGWoZnXjeJMhd2ZiTVuxO|c2 NFizcGQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEG3PVE2Oid-MkSxO|kyPTJ:L3G+
THP-1 NIPzO4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX[wMlAyOeLCk{ig{txO MUG5OkBp NYPHcJRC\W6qYX7j[ZMhfGinIHHueIlxem:uaX\ldoF1cX[nIHXm[oVkfHNib3[gUWsyPzd3 MoriQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRzN{mxOVIoRjJ2MUe5NVUzRC:jPh?=
HL-60  NV;hc2N2TnWwY4Tpc44hSXO|YYm= MV[xNEBuVQ>? M3HoTVAvPSCq NVG4V4RVemWmdXPld{BxcG:|cHjvdplt[XSrb36gc4YhS2itMTDheEB{\XKrbnWgN|Q2 MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl|NESxNUc,OjN7M{S0NVE9N2F-
OVCAR-8  Ml72SpVv[3Srb36gRZN{[Xl? NVzsdYlwOSEEtV5CpC=> NXGzeodMOjRiaB?= MnfzZYJzd2ejdHXzJINp\W2xdHjldoFxgS2rbnT1Z4VlKGOnbHygZ5lkdGViYYLy[ZN1 MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzV2OEK2PUc,OjN3NEiyOlk9N2F-
PANC-1 M3\VdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\WO|AvOTFvOTFOwG0> MXqxJIg> M4\ES4lvcGmkaYTzJJRp\SClZXzsJJZq[WKrbHn0fUBqdiCjIHTvd4UuKGSncHXu[IVvfCCvYX7u[ZI> MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjh{NUOzNUc,OjJ6MkWzN|E9N2F-
MiaPaCa Mlj1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELkXpcxNjFzLUmg{txO MlfmNUBp NFK3c21qdmirYnn0d{B1cGViY3XscEB3cWGkaXzpeJkhcW5iYTDkc5NmNSCmZYDlcoRmdnRibXHucoVz MlvmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ6MkWzN|EoRjJ{OEK1N|MyRC:jPh?=
PSN-1 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYK2XVJNOC5zMT25JO69VQ>? NFG3Zm4yKGh? NWnhcWhrcW6qaXLpeJMhfGinIHPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S1iZHXw[Y5l\W62IH3hco5meg>? M1nye|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{OEK1N|MyLz5{MkiyOVM{OTxxYU6=
K562 NYHxXZgxSXCxcITvd4l{KGG|c3H5 MliyNVAhfU1? NEj5R401QCCqcoO= MUTJcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIHj1cYFvKEt3NkKgZ4VtdHNiYYPz[ZN{\WRiYYOg[4FudWGKMlHYM|U{SlBzIHzleoVteyCjdDCxNEB2VSCjZoTldkA1QCCqcoOgZpkhTEGSSTDzeIFqdmmwZzDiZZNm\CCrbX31co9ndHWxcnXzZ4Vv[2VibXnjdo9{[2:yeTDpckBxemW|ZX7j[UBw\iB{NTD0c{AzPTBicF2gLE0qNWyxbXHpeol1cWOrbjDB MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzF5N{iyOkc,OjdzN{e4NlY9N2F-
SJ-GBM2 Mn;ydWhVWyCjc4PhfS=> NFfQTYFyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1qtS2JOOiClZXzsdy=> NY\TdGRjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-MC Mo\QdWhVWyCjc4PhfS=> NWrlRY5PeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPLMW4uVUNiY3XscJM> MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
MDCK M1HSOWN6fG:2b4jpZ4l1gSCjc4PhfS=> NGD6WY42ODBibl2= NYfqO4c1OSCqch?= MXTDfZRwfG:6aXPpeJkh[WejaX7zeEBOTEONIHPlcIx{KGW6cILld5NqdmdiY3HyZo9vcWNiYX7ofYRz[XOnIEmgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KGG2IEWwNEBvVSCycnX0doVifGWmIH\vdkAyKGi{IH\vcIxwf2WmIHL5JFIhT3liaYLyZYRq[XSrb36geY5l\XJibn;ycY95cWNiY3;u[Il1cW:wIHL5JGFt[W2jcjDicJVmKGG|c3H5 MomzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd6MkO4O|koRjJ5OEKzPFc6RC:jPh?=
MDCK NYfQVoJmS3m2b4TvfIlkcXS7IHHzd4F6 NWG3SIQ1PTByIH7N NVHtUIFlOSCqch?= MYjDfZRwfG:6aXPpeJkh[WejaX7zeEBOTEONIHPlcIx{KGW6cILld5NqdmdiY3HyZo9vcWNiYX7ofYRz[XOnIEmgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KGG2IEWwNEBvVSCycnX0doVifGWmIH\vdkAyKGi{IH\vcIxwf2WmIHL5JFQhT3liaYLyZYRq[XSrb36geY5l\XJiYX7vfIlkKGOxbnTpeIlwdiCkeTDBcIFu[XJiYnz1[UBie3OjeR?= Mn7uQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd6MkO4O|koRjJ5OEKzPFc6RC:jPh?=
MDCK MofjR5l1d3SxeHnjbZR6KGG|c3H5 Ml32OVAxKG6P NFPWZlg4OiCqcoO= NX\ielVOS3m2b4TvfIlkcXS7IHHnZYlve3RiTVTDT{Bk\WyuczDlfJBz\XO|aX7nJINiemKxbnnjJIFvcHmmcnHz[UA6KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBk\WyuII\pZYJqdGm2eTDheEA2ODBibl2gdJJmfHKnYYTl[EBnd3JiN{KgbJJ{KG[xbHzve4VlKGK7IEeyJIhzeyCrbnP1ZoF1cW:wIIXu[IVzKG6xcn3vfIlkKGOxbnTpeIlwdiCkeTDBcIFu[XJiYnz1[UBie3OjeR?= M2D1dlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5OEKzPFc6Lz5{N{iyN|g4QTxxYU6=
MDCK MWTDfZRwfG:6aXPpeJkh[XO|YYm= MX21NFAhdk1? M{juO|czKGi{cx?= MYPDfZRwfG:6aXPpeJkh[WejaX7zeEBOTEONIHPlcIx{KGW6cILld5NqdmdiY3HyZo9vcWNiYX7ofYRz[XOnIEmgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIHPlcIwhfmmjYnnsbZR6KGG2IEWwNEBvVSCjZoTldkA4OiCqcoOgeY5l\XJiYX7vfIlkKGOxbnTpeIlwdiCkeTDBcIFu[XJiYnz1[UBie3OjeR?= NUm5eW1yRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke4NlM5PzlpPkK3PFI{QDd7PD;hQi=>
Assay
Methods Test Index PMID
Western blot p-AKT / AKT / p-ERK / ERK ; Vimentin ; E-cadherin / Vimentin / ZEB1 29157079
Growth inhibition assay Cell viability 29157079

Protocol (from reference)

Kinase Assay:

[2]

  • Kinase inhibition:

    The ability of compounds to inhibit ATR, ATM or DNAPK kinase activity istested using a radiometric-phosphate incorporation assay. A stock solution isprepared consisting of the appropriate buffer, kinase, and target peptide. To this isadded the compound of interest, at varying concentrations in DMSO to a final DMSO concentration of 7%. Assays are initiated by addition of an appropriate [γ-33P]ATP solution and incubated at 25 ℃. Assays are stopped, after the desired time course, by addition of phosphoric acid and ATP to a final concentration of 100 mM and 0.66μM, respectively. Peptides are captured on a phosphocellulose membrane, prepared as per manufacturer

Cell Research:

[2]

  • Cell lines: H2AX cells
  • Concentrations: --
  • Incubation Time: 96 hours
  • Method:

    Cells are plated in 96-well plates and allowed to adhere overnight. The following day, compounds are added at the indicated concentrations in a final volume of 200μL, and the cells are then incubated for 96 h. MTS reagent (40μL) isthen added, and 1 h later, absorbance at 490 nm ismeasured using a SpectraMax Plus 384 plate reader. Synergy and antagonism are assessed using Macsynergy software.

Solubility (25°C)

In vitro

DMSO 74 mg/mL
(200.86 mM)
Water Insoluble
Ethanol Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing.

30 mg/mL

Chemical Information

Molecular Weight 368.41
Formula

C18H16N4O3S

CAS No. 1232410-49-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CS(=O)(=O)C1=CC=C(C=C1)C2=CN=C(C(=N2)C(=O)NC3=CC=CC=C3)N

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

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