Catalog No.S8007

VE-821 Chemical Structure

Molecular Weight(MW): 368.41

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.

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Cited by 28 Publications

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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.
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  M3\XWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{TXTWlEPTExv[6wMlgh|ryP NIe1bHgzPTV7M{G4OC=>
SAOS2 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|Ux973gMD64JO69VQ>? MV[yOVU6OzF6NB?=
CAL72 NEnzWYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|Ux973gMD64JO69VQ>? Ml3YNlU2QTNzOES=
NOS1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|Ux973gMD64JO69VQ>? M4m1XFI2PTl|MUi0
HUO9 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|Ux973gMD64JO69VQ>? NF;QSJIzPTV7M{G4OC=>
MG63 NE\GOoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjnNWlKSzVy784ePUDPxE1? NW[2do5WOjV3OUOxPFQ>
SJSA1 NWrOT4JbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDWSot7UUN3MP-9olkh|ryP M3\N[VI2PTl|MUi0
MDA-MB-231 NXq2RZlxS3m2b4TvfIlkcXS7IFHzd4F6 MWqxM|MwOTBizszN MXOxJIg> M2rtOJBwfGWwdHnheIV{KHSqZTDjfZRwfG:6aXPpeJkhd2ZiYn;0bEBk[W2ydH;0bIVkcW5iYX7kJGxOWC12MEC= MmrpNlUzPjl2N{m=
HT-29 MYrDfZRwfG:6aXPpeJkhSXO|YYm= NXHaXJJjOS9|L{GwJO69VQ>? MXixJIg> NV23WmpZeG:2ZX70bYF1\XNidHjlJIN6fG:2b4jpZ4l1gSCxZjDic5RpKGOjbYD0c5Rp\WOrbjDhcoQhVE2SLUSwNC=> MkPiNlUzPjl2N{m=
HCT-116 p53+/+ MVTDfZRwfG:6aXPpeJkhSXO|YYm= MkPINU8{NzFyIN88US=> M17mZ|EhcA>? MkG1dI91\W62aXH0[ZMhfGinIHP5eI91d3irY3n0fUBw\iCkb4ToJINidXC2b4To[YNqdiCjbnSgUG1RNTRyMB?= M4jQdFI2OjZ7NEe5
HCT-116 p53-/- MX\DfZRwfG:6aXPpeJkhSXO|YYm= MnjRNU8{NzFyIN88US=> M1PxRVEhcA>? M3nkO5BwfGWwdHnheIV{KHSqZTDjfZRwfG:6aXPpeJkhd2ZiYn;0bEBk[W2ydH;0bIVkcW5iYX7kJGxOWC12MEC= M2nWO|I2OjZ7NEe5
TF-1 NXPHRmpTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;WWoZwOC5yMUJihLM5KM7:TR?= NHrXdng6PiCq NXzFS5Br\W6qYX7j[ZMhfGinIHHueIlxem:uaX\ldoF1cX[nIHXm[oVkfHNib3[gUWsyPzd3 MVOyOFE4QTF3Mh?=
HEL MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NISzUnkxNjBzMfMAl|gh|ryP NFTnZo46PiCq Mmry[Y5p[W6lZYOgeIhmKGGwdHnwdo9tcW[ncnH0bZZmKGWoZnXjeJMhd2ZiTVuxO|c2 MWqyOFE4QTF3Mh?=
THP-1 NYTRU|E5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYmwMlAyOeLCk{ig{txO NVXtNXpVQTZiaB?= M{T5eoVvcGGwY3XzJJRp\SCjboTpdJJwdGmoZYLheIl3\SCnZn\lZ5R{KG:oIF3LNVc4PQ>? M4n6clI1OTd7MUWy
HL-60  MV3GeY5kfGmxbjDBd5NigQ>? NV[xdlFMOTBibV2= NFPaRpoxNjViaB?= M2XJSJJm\HWlZYOgdIhwe3Cqb4L5cIF1cW:wIH;mJGNpczFiYYSgd4VzcW6nIEO0OS=> MYqyN|k{PDRzMR?=
OVCAR-8  NGfY[4RHfW6ldHnvckBCe3OjeR?= NXWwRWxCOSEEtV5CpC=> M13zNlI1KGh? M{fNO4Fjem:pYYTld{BkcGWvb4To[ZJieHlvaX7keYNm\CClZXzsJIN6[2ynIHHydoV{fA>? M2iwUFI{PTR6Mk[5
PANC-1 NEDZNHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmizNE4yOS17IN88US=> MoP5NUBp M3\hSIlvcGmkaYTzJJRp\SClZXzsJJZq[WKrbHn0fUBqdiCjIHTvd4UuKGSncHXu[IVvfCCvYX7u[ZI> NYjoNlR2OjJ6MkWzN|E>
MiaPaCa M1izZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjINE4yOS17IN88US=> MmL6NUBp MY\pcohq[mm2czD0bIUh[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlMUBl\XCnbnTlcpQhdWGwbnXy MWCyNlgzPTN|MR?=
PSN-1 Ml3BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDTU4IxNjFzLUmg{txO NWPhNlM4OSCq M2LFNIlvcGmkaYTzJJRp\SClZXzsJJZq[WKrbHn0fUBqdiCjIHTvd4UuKGSncHXu[IVvfCCvYX7u[ZI> MlP3NlI5OjV|M{G=

... Click to View More Cell Line Experimental Data


Kinase Assay:


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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:


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  • 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.

    (Only for Reference)

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

* 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 368.41


CAS No. 1232410-49-9
Storage powder
in solvent
Synonyms N/A

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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID