For research use only.

Catalog No.S8007

126 publications

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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10mM (1mL in DMSO) EUR 187 In stock
EUR 144 In stock
EUR 461 In stock
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Selleck's VE-821 has been cited by 126 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  MoHNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|Ux973gMD64JO69VQ>? NGX1eY8zPTV7M{G4OC=>
SAOS2 Mnj1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|Ux973gMD64JO69VQ>? M{jBTVI2PTl|MUi0
CAL72 MoDvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXG[|BKSzVy784eNE45KM7:TR?= M4ToSFI2PTl|MUi0
NOS1 NIr3VIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\kcXZOUUN3MP-9olAvQCEQvF2= M3fqblI2PTl|MUi0
HUO9 MkGwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTWTWM2OO,;nkCuPEDPxE1? MV:yOVU6OzF6NB?=
MG63 NVizbWNCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3OwTGlEPTExv[65JO69VQ>? MVWyOVU6OzF6NB?=
SJSA1 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXu4VW15UUN3MP-9olkh|ryP M{Th[VI2PTl|MUi0
MDA-MB-231 M{\Pd2N6fG:2b4jpZ4l1gSCDc4PhfS=> MX2xM|MwOTBizszN NGDSco8yKGh? MVLwc5RmdnSrYYTld{B1cGViY4n0c5RwgGmlaYT5JI9nKGKxdHigZ4FueHSxdHjlZ4lvKGGwZDDMUXAuPDBy NWfLSZJuOjV{Nkm0O|k>
HT-29 M2Cx[mN6fG:2b4jpZ4l1gSCDc4PhfS=> MUGxM|MwOTBizszN NH7jWIIyKGh? M4f4fJBwfGWwdHnheIV{KHSqZTDjfZRwfG:6aXPpeJkhd2ZiYn;0bEBk[W2ydH;0bIVkcW5iYX7kJGxOWC12MEC= MVGyOVI3QTR5OR?=
HCT-116 p53+/+ NGfhd2ZEgXSxdH;4bYNqfHliQYPzZZk> NXvmeJZ4OS9|L{GwJO69VQ>? NEHPRZQyKGh? NWOyOZdLeG:2ZX70bYF1\XNidHjlJIN6fG:2b4jpZ4l1gSCxZjDic5RpKGOjbYD0c5Rp\WOrbjDhcoQhVE2SLUSwNC=> NUjvUGFEOjV{Nkm0O|k>
HCT-116 p53-/- NWfrRW9XS3m2b4TvfIlkcXS7IFHzd4F6 MknpNU8{NzFyIN88US=> MUGxJIg> NVHkT2lEeG:2ZX70bYF1\XNidHjlJIN6fG:2b4jpZ4l1gSCxZjDic5RpKGOjbYD0c5Rp\WOrbjDhcoQhVE2SLUSwNC=> NYT3fFh1OjV{Nkm0O|k>
TF-1 M4jrNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFrHe|MxNjBzMfMAl|gh|ryP M{PTd|k3KGh? NIP4U5RmdmijbnPld{B1cGViYX70bZBzd2yrZnXyZZRqfmViZX\m[YN1eyCxZjDNT|E4PzV? Ml;DNlQyPzlzNUK=
HEL NFvJd5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4npOlAvODFz4pETPEDPxE1? MnvXPVYhcA>? M1zufIVvcGGwY3XzJJRp\SCjboTpdJJwdGmoZYLheIl3\SCnZn\lZ5R{KG:oIF3LNVc4PQ>? NVPSRpJZOjRzN{mxOVI>
THP-1 MnPDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LHbFAvODFz4pETPEDPxE1? MUC5OkBp NFnuZWtmdmijbnPld{B1cGViYX70bZBzd2yrZnXyZZRqfmViZX\m[YN1eyCxZjDNT|E4PzV? MYCyOFE4QTF3Mh?=
HL-60  NVTBTYRYTnWwY4Tpc44hSXO|YYm= NVjwVY1jOTBibV2= MlWxNE42KGh? NHP5R3hz\WS3Y3XzJJBpd3OyaH;yfYxifGmxbjDv[kBEcGtzIHH0JJNmemmwZTCzOFU> MnnmNlM6OzR2MUG=
OVCAR-8  NX3mcGpnTnWwY4Tpc44hSXO|YYm= MVexJOK2VcLi M4\IVlI1KGh? MnixZYJzd2ejdHXzJINp\W2xdHjldoFxgS2rbnT1Z4VlKGOnbHygZ5lkdGViYYLy[ZN1 M3rm[lI{PTR6Mk[5
PANC-1 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTENE4yOS17IN88US=> NGO5[28yKGh? NXHMXmEzcW6qaXLpeJMhfGinIHPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S1iZHXw[Y5l\W62IH3hco5meg>? MUOyNlgzPTN|MR?=
MiaPaCa MknpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;ETFAvOTFvOTFOwG0> MX:xJIg> NXyxT29kcW6qaXLpeJMhfGinIHPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S1iZHXw[Y5l\W62IH3hco5meg>? Mnv3NlI5OjV|M{G=
PSN-1 M{HQcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU[wMlEyNTlizszN NWnXXpJPOSCq MoXhbY5pcWKrdIOgeIhmKGOnbHygeoli[mmuaYT5JIlvKGFiZH;z[U0h\GWyZX7k[Y51KG2jbn7ldi=> Mn3vNlI5OjV|M{G=

... 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