VE-821

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 68 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.
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  MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDGc41KSzVy784eNE45KM7:TR?= MVuyOVU6OzF6NB?=
SAOS2 M3i1ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojNTWM2OO,;nkCuPEDPxE1? MXWyOVU6OzF6NB?=
CAL72 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3XjdGlEPTExv[6wMlgh|ryP M1Gzb|I2PTl|MUi0
NOS1 M{nIPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjRR|FKSzVy784eNE45KM7:TR?= NXX2d2ZHOjV3OUOxPFQ>
HUO9 MojHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|Ux973gMD64JO69VQ>? NEW1SFEzPTV7M{G4OC=>
MG63 MlTRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|Ux973gOTFOwG0> NUPwR4cyOjV3OUOxPFQ>
SJSA1 Mo\LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3zUSWlEPTExv[65JO69VQ>? Mli4NlU2QTNzOES=
MDA-MB-231 NIfmcGREgXSxdH;4bYNqfHliQYPzZZk> MkfvNU8{NzFyIN88US=> M4rnRlEhcA>? NWDiXnR{eG:2ZX70bYF1\XNidHjlJIN6fG:2b4jpZ4l1gSCxZjDic5RpKGOjbYD0c5Rp\WOrbjDhcoQhVE2SLUSwNC=> M2TORlI2OjZ7NEe5
HT-29 Mlr5R5l1d3SxeHnjbZR6KEG|c3H5 MnjiNU8{NzFyIN88US=> MknvNUBp MX\wc5RmdnSrYYTld{B1cGViY4n0c5RwgGmlaYT5JI9nKGKxdHigZ4FueHSxdHjlZ4lvKGGwZDDMUXAuPDBy NGrH[JUzPTJ4OUS3PS=>
HCT-116 p53+/+ NVjhZWg5S3m2b4TvfIlkcXS7IFHzd4F6 NHXyTJAyNzNxMUCg{txO MVGxJIg> NHrrWYJxd3SnboTpZZRmeyC2aHWgZ5l1d3SxeHnjbZR6KG:oIHLveIgh[2GvcITveIhm[2mwIHHu[EBNVVBvNECw MWWyOVI3QTR5OR?=
HCT-116 p53-/- M4XVWmN6fG:2b4jpZ4l1gSCDc4PhfS=> NHjCTWUyNzNxMUCg{txO MkLlNUBp NXfkPYh4eG:2ZX70bYF1\XNidHjlJIN6fG:2b4jpZ4l1gSCxZjDic5RpKGOjbYD0c5Rp\WOrbjDhcoQhVE2SLUSwNC=> NUn0VXJKOjV{Nkm0O|k>
TF-1 NF:2b2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUi1bWtIOC5yMUJihLM5KM7:TR?= MXS5OkBp NHKzTohmdmijbnPld{B1cGViYX70bZBzd2yrZnXyZZRqfmViZX\m[YN1eyCxZjDNT|E4PzV? MYeyOFE4QTF3Mh?=
HEL NWTtN5lHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYqwMlAyOeLCk{ig{txO MUW5OkBp MkPF[Y5p[W6lZYOgeIhmKGGwdHnwdo9tcW[ncnH0bZZmKGWoZnXjeJMhd2ZiTVuxO|c2 MYKyOFE4QTF3Mh?=
THP-1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{LTZ|AvODFz4pETPEDPxE1? M2nnWVk3KGh? MVjlcohidmOnczD0bIUh[W62aYDyc4xq\mW{YYTpeoUh\W[oZXP0d{Bw\iCPS{G3O|U> NVPRfXVoOjRzN{mxOVI>
HL-60  MU\GeY5kfGmxbjDBd5NigQ>? MmrlNVAhdU1? MlfBNE42KGh? MUXy[YR2[2W|IIDoc5NxcG:{eXzheIlwdiCxZjDDbIsyKGG2IIPldolv\SB|NEW= NHXp[W4zOzl|NESxNS=>
OVCAR-8  M2jpbWZ2dmO2aX;uJGF{e2G7 Mkm0NUDDvU4EoB?= MVSyOEBp NEnDb29i[nKxZ3H0[ZMh[2inbX;0bIVz[XC7LXnu[JVk\WRiY3XscEBkgWOuZTDhdpJme3R? M4S2cFI{PTR6Mk[5
PANC-1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV2wMlEyNTlizszN NFrI[YEyKGh? M4TVTIlvcGmkaYTzJJRp\SClZXzsJJZq[WKrbHn0fUBqdiCjIHTvd4UuKGSncHXu[IVvfCCvYX7u[ZI> MVmyNlgzPTN|MR?=
MiaPaCa M{XjVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjDNE4yOS17IN88US=> MYOxJIg> MWjpcohq[mm2czD0bIUh[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlMUBl\XCnbnTlcpQhdWGwbnXy M1fRcFIzQDJ3M{Ox
PSN-1 NX7GTW03T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfKNE4yOS17IN88US=> MkXFNUBp NEPMfIFqdmirYnn0d{B1cGViY3XscEB3cWGkaXzpeJkhcW5iYTDkc5NmNSCmZYDlcoRmdnRibXHucoVz NYjZcVRpOjJ6MkWzN|E>

... Click to View More Cell Line Experimental Data

Assay
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.

Vimentin; 

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.

29157079
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.

29157079

Protocol

Kinase Assay:

[2]

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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:

[2]

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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
Formula

C18H16N4O3S

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID