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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4 Customer Reviews

  • Cell viability response to ATR inhibitor.

    Nature, 2018, 555(7696):387-391. VE-821 purchased from Selleck.

    (C) VCaP cells were treated with T-474 together with the ATR inhibitor VE-821, ATM inhibitor KU-55933, or DNA-PK inhibitor NU7026 as indicated for 4 days. Cell viability was measured (N = 3, mean with SD). *P < 0.01 and **P < 0.000001; N.S., not significant (P > 0.05).

    Oncotarget, 2018, 9(17): 13474-13487. VE-821 purchased from Selleck.

  • Western blot analysis of phospho-p53 and total p53 in H1 cells treated with 2 uM MNNG and the ATM-specific inhibitor KU5593, the ATR-specific inhibitor VE-821, or both for 24 h. The values represent the means of three independent experiments. Error bars represent S.E.

    J Biol Chem 2014 289(35), 24314-24. VE-821 purchased from Selleck.

    Western blot for γH2AX in H460 cells treated with Cr(VI) in the presence of a second set of inhibitors (ATM-i2—10 uM KU55933, DNAPK-i2—10 uM NU7441, ATR-i2—10 uM VE821). “γH2AX-total” numbers indicate a total normalized intensity of both γH2AX bands from 2 Western blots.

    Toxicol Sci 2014 10.1093/toxsci/kfu207. VE-821 purchased from Selleck.

Purity & Quality Control

Choose Selective ATM/ATR Inhibitors

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  MlrkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInEW4dKSzVy784eNE45KM7:TR?= MY[yOVU6OzF6NB?=
SAOS2 M1OyZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUS4fpNFUUN3MP-9olAvQCEQvF2= NUHEeWtKOjV3OUOxPFQ>
CAL72 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mkf0TWM2OO,;nkCuPEDPxE1? MknsNlU2QTNzOES=
NOS1 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTIT|R7UUN3MP-9olAvQCEQvF2= NFiwfpgzPTV7M{G4OC=>
HUO9 NXnDflRsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjIZ|VzUUN3MP-9olAvQCEQvF2= NV3rZZptOjV3OUOxPFQ>
MG63 MoL1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|Ux973gOTFOwG0> M3LIXVI2PTl|MUi0
SJSA1 NWHyTI5ZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTYNWE6UUN3MP-9olkh|ryP MliwNlU2QTNzOES=
MDA-MB-231 Ml2wR5l1d3SxeHnjbZR6KEG|c3H5 MXexM|MwOTBizszN NWHufZFsOSCq NYLr[nJUeG:2ZX70bYF1\XNidHjlJIN6fG:2b4jpZ4l1gSCxZjDic5RpKGOjbYD0c5Rp\WOrbjDhcoQhVE2SLUSwNC=> MWKyOVI3QTR5OR?=
HT-29 M4DE[WN6fG:2b4jpZ4l1gSCDc4PhfS=> NGS3b2UyNzNxMUCg{txO NFexdVMyKGh? MU\wc5RmdnSrYYTld{B1cGViY4n0c5RwgGmlaYT5JI9nKGKxdHigZ4FueHSxdHjlZ4lvKGGwZDDMUXAuPDBy NFPWdm8zPTJ4OUS3PS=>
HCT-116 p53+/+ M2fne2N6fG:2b4jpZ4l1gSCDc4PhfS=> NHnYUZAyNzNxMUCg{txO M3jJVlEhcA>? NWjrXpZQeG:2ZX70bYF1\XNidHjlJIN6fG:2b4jpZ4l1gSCxZjDic5RpKGOjbYD0c5Rp\WOrbjDhcoQhVE2SLUSwNC=> NH7sOIozPTJ4OUS3PS=>
HCT-116 p53-/- M{DWbWN6fG:2b4jpZ4l1gSCDc4PhfS=> NX\zOXhuOS9|L{GwJO69VQ>? NUjXUIJiOSCq NYPpZpd2eG:2ZX70bYF1\XNidHjlJIN6fG:2b4jpZ4l1gSCxZjDic5RpKGOjbYD0c5Rp\WOrbjDhcoQhVE2SLUSwNC=> NX3Zb5lMOjV{Nkm0O|k>
TF-1 M{D5bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnhN4pGOC5yMUJihLM5KM7:TR?= M174eVk3KGh? MVrlcohidmOnczD0bIUh[W62aYDyc4xq\mW{YYTpeoUh\W[oZXP0d{Bw\iCPS{G3O|U> MknLNlQyPzlzNUK=
HEL MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUSxZmxPOC5yMUJihLM5KM7:TR?= NGfTfoU6PiCq NYO3O5J{\W6qYX7j[ZMhfGinIHHueIlxem:uaX\ldoF1cX[nIHXm[oVkfHNib3[gUWsyPzd3 Ml7TNlQyPzlzNUK=
THP-1 NVntcINRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlL1NE4xOTIkgKO4JO69VQ>? NVi0R|g5QTZiaB?= M{HYVIVvcGGwY3XzJJRp\SCjboTpdJJwdGmoZYLheIl3\SCnZn\lZ5R{KG:oIF3LNVc4PQ>? MoLONlQyPzlzNUK=
HL-60  NX3OdpAzTnWwY4Tpc44hSXO|YYm= NHv5e5EyOCCvTR?= MWmwMlUhcA>? NXvvenExemWmdXPld{BxcG:|cHjvdplt[XSrb36gc4YhS2itMTDheEB{\XKrbnWgN|Q2 NFnzcnczOzl|NESxNS=>
OVCAR-8  MYXGeY5kfGmxbjDBd5NigQ>? MmDNNUDDvU4EoB?= MmT5NlQhcA>? MoXEZYJzd2ejdHXzJINp\W2xdHjldoFxgS2rbnT1Z4VlKGOnbHygZ5lkdGViYYLy[ZN1 MXKyN|U1QDJ4OR?=
PANC-1 MojhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjDNlcxNjFzLUmg{txO MV[xJIg> NGGwbmFqdmirYnn0d{B1cGViY3XscEB3cWGkaXzpeJkhcW5iYTDkc5NmNSCmZYDlcoRmdnRibXHucoVz M1fic|IzQDJ3M{Ox
MiaPaCa M1nGUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHpUWIxNjFzLUmg{txO MmnmNUBp M4q3UYlvcGmkaYTzJJRp\SClZXzsJJZq[WKrbHn0fUBqdiCjIHTvd4UuKGSncHXu[IVvfCCvYX7u[ZI> NFHqb4IzOjh{NUOzNS=>
PSN-1 MmDlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfu[mJLOC5zMT25JO69VQ>? NYTNb4Q3OSCq NVHEW5FFcW6qaXLpeJMhfGinIHPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S1iZHXw[Y5l\W62IH3hco5meg>? NYC4WoJjOjJ6MkWzN|E>

... Click to View More Cell Line Experimental Data

Protocol

Kinase Assay:

[2]

+ Expand

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]

+ Expand
  • 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

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

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  • Computed Result

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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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

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID