For research use only.

Catalog No.S8007

139 publications

VE-821 Chemical Structure

CAS No. 1232410-49-9

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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10mM (1mL in DMSO) USD 191 In stock
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Selleck's VE-821 has been cited by 139 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  MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzZcIRKUUN3MP-9olAvQCEQvF2= Moj1NlU2QTNzOES=
SAOS2 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVL0T41FUUN3MP-9olAvQCEQvF2= NXz5dVl[OjV3OUOxPFQ>
CAL72 MoPOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jWT2lEPTExv[6wMlgh|ryP M1\ncFI2PTl|MUi0
NOS1 Mk\2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX75eWdXUUN3MP-9olAvQCEQvF2= MXWyOVU6OzF6NB?=
HUO9 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1vB[mlEPTExv[6wMlgh|ryP M2DPWFI2PTl|MUi0
MG63 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\IWXhzUUN3MP-9olkh|ryP NUnPXoYyOjV3OUOxPFQ>
SJSA1 NUD3bG5bT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|Ux973gOTFOwG0> MXmyOVU6OzF6NB?=
HT-29 MnLBR5l1d3SxeHnjbZR6KEG|c3H5 MknYNU8{NzFyIN88US=> M3zROFEhcA>? M4Xze5BwfGWwdHnheIV{KHSqZTDjfZRwfG:6aXPpeJkhd2ZiYn;0bEBk[W2ydH;0bIVkcW5iYX7kJGxOWC12MEC= MoraNlUzPjl2N{m=
HCT-116 p53+/+ NXPPV4s4S3m2b4TvfIlkcXS7IFHzd4F6 MYOxM|MwOTBizszN NVHNdm1yOSCq MXLwc5RmdnSrYYTld{B1cGViY4n0c5RwgGmlaYT5JI9nKGKxdHigZ4FueHSxdHjlZ4lvKGGwZDDMUXAuPDBy MXyyOVI3QTR5OR?=
HCT-116 p53-/- MVrDfZRwfG:6aXPpeJkhSXO|YYm= MnfFNU8{NzFyIN88US=> NV;mfGtXOSCq MXvwc5RmdnSrYYTld{B1cGViY4n0c5RwgGmlaYT5JI9nKGKxdHigZ4FueHSxdHjlZ4lvKGGwZDDMUXAuPDBy NHezNmUzPTJ4OUS3PS=>
HEL M2XW[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH2w[oExNjBzMfMAl|gh|ryP NH3FOIM6PiCq NYXoNI1n\W6qYX7j[ZMhfGinIHHueIlxem:uaX\ldoF1cX[nIHXm[oVkfHNib3[gUWsyPzd3 M3u2cVI1OTd7MUWy
THP-1 MlHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXmwMlAyOeLCk{ig{txO Mm\FPVYhcA>? Mlvj[Y5p[W6lZYOgeIhmKGGwdHnwdo9tcW[ncnH0bZZmKGWoZnXjeJMhd2ZiTVuxO|c2 NFHuTpozPDF5OUG1Ni=>
HL-60  NVPKSHFpTnWwY4Tpc44hSXO|YYm= NF6yPVgyOCCvTR?= M4f1W|AvPSCq MmrYdoVlfWOnczDwbI9{eGixconsZZRqd25ib3[gR4hsOSCjdDDz[ZJqdmViM{S1 NHrnPJgzOzl|NESxNS=>
OVCAR-8  M2DDUWZ2dmO2aX;uJGF{e2G7 M2LRXlEhyrWPwrC= NUSxcmNGOjRiaB?= MorWZYJzd2ejdHXzJINp\W2xdHjldoFxgS2rbnT1Z4VlKGOnbHygZ5lkdGViYYLy[ZN1 M3O4SFI{PTR6Mk[5
PANC-1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUGwMlEyNTlizszN M2DPfVEhcA>? NVLGfGp7cW6qaXLpeJMhfGinIHPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S1iZHXw[Y5l\W62IH3hco5meg>? NFy0bG4zOjh{NUOzNS=>
MiaPaCa MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\uNE4yOS17IN88US=> M3jNdFEhcA>? NIrHSpNqdmirYnn0d{B1cGViY3XscEB3cWGkaXzpeJkhcW5iYTDkc5NmNSCmZYDlcoRmdnRibXHucoVz M4LVXVIzQDJ3M{Ox
PSN-1 M1vnZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3e3NlAvOTFvOTFOwG0> MWGxJIg> NUHLR5pqcW6qaXLpeJMhfGinIHPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S1iZHXw[Y5l\W62IH3hco5meg>? NFXiR5AzOjh{NUOzNS=>

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
E-cadherin / Vimentin / ZEB1 ; 

PubMed: 29157079     

Four kinds of cancer cells were treated with 5 μM VE-821 for 24 h and 48 h. The expression of E-cadherin, Vimentin and ZEB1 was performed by Western Blotting. Actin was used as loading control.


PubMed: 29157079     

(D) MGC-803 cells were stained with antibodies to Vimentin (green) and nuclei was stained with DAPI. Images were captured by fluorescence microscopy at × 40 magnification.

p-AKT / AKT / p-ERK / ERK ; 

PubMed: 29157079     

HCT-116 and NCI-N87 cells were added to 5 μM VE-821 for 24 h and 48 h. The total and phosphorylation expression of AKT and ERK was performed by Western Blotting.

Growth inhibition assay
Cell viability; 

PubMed: 29157079     

Indicated concentrations of VE-821 (0, 1, 5 and 10 μM) were added to four kinds of cancer cells (PANC-1, MGC-803, HCT-116 and NCI-N87) for 48 h. Cell viability was performed by MTT assay. Results from three independent experiments are shown.



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
Smiles CS(=O)(=O)C1=CC=C(C=C1)C2=CN=C(C(=N2)C(=O)NC3=CC=CC=C3)N

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID