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.

Size Price Stock Quantity  
USD 147 In stock
USD 470 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Cited by 51 Publications

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  M2nabmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\hPJl1UUN3MP-9olAvQCEQvF2= MVOyOVU6OzF6NB?=
SAOS2 NVW2eIZ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnG0TWM2OO,;nkCuPEDPxE1? NXjZOXdEOjV3OUOxPFQ>
CAL72 MmrxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|Ux973gMD64JO69VQ>? MWCyOVU6OzF6NB?=
NOS1 NWD2W3IxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlLLTWM2OO,;nkCuPEDPxE1? MVeyOVU6OzF6NB?=
HUO9 Ml\pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HSUGlEPTExv[6wMlgh|ryP MYqyOVU6OzF6NB?=
MG63 NYq4WpJ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|Ux973gOTFOwG0> MXqyOVU6OzF6NB?=
SJSA1 NVHpN4Z1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3nSO2lEPTExv[65JO69VQ>? NI\FcIYzPTV7M{G4OC=>
MDA-MB-231 NVLBZnhFS3m2b4TvfIlkcXS7IFHzd4F6 M4HRNlEwOy9zMDFOwG0> MYCxJIg> NWTVZZdweG:2ZX70bYF1\XNidHjlJIN6fG:2b4jpZ4l1gSCxZjDic5RpKGOjbYD0c5Rp\WOrbjDhcoQhVE2SLUSwNC=> NHLNbXEzPTJ4OUS3PS=>
HT-29 M{[5fmN6fG:2b4jpZ4l1gSCDc4PhfS=> NGLpdFgyNzNxMUCg{txO MXKxJIg> MoPOdI91\W62aXH0[ZMhfGinIHP5eI91d3irY3n0fUBw\iCkb4ToJINidXC2b4To[YNqdiCjbnSgUG1RNTRyMB?= MV:yOVI3QTR5OR?=
HCT-116 p53+/+ NGj6dIFEgXSxdH;4bYNqfHliQYPzZZk> M4Ttd|EwOy9zMDFOwG0> NIXWW4IyKGh? MkTvdI91\W62aXH0[ZMhfGinIHP5eI91d3irY3n0fUBw\iCkb4ToJINidXC2b4To[YNqdiCjbnSgUG1RNTRyMB?= NY\2N3c2OjV{Nkm0O|k>
HCT-116 p53-/- NFvWS4lEgXSxdH;4bYNqfHliQYPzZZk> M2jTW|EwOy9zMDFOwG0> NIXVe|QyKGh? MmO5dI91\W62aXH0[ZMhfGinIHP5eI91d3irY3n0fUBw\iCkb4ToJINidXC2b4To[YNqdiCjbnSgUG1RNTRyMB?= NFzVWJYzPTJ4OUS3PS=>
TF-1 MoroS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorqNE4xOTIkgKO4JO69VQ>? NU\QcIx{QTZiaB?= NY\iSGJi\W6qYX7j[ZMhfGinIHHueIlxem:uaX\ldoF1cX[nIHXm[oVkfHNib3[gUWsyPzd3 NFvNVmozPDF5OUG1Ni=>
HEL MoPnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jO[|AvODFz4pETPEDPxE1? NEHv[mY6PiCq NWDXNIxQ\W6qYX7j[ZMhfGinIHHueIlxem:uaX\ldoF1cX[nIHXm[oVkfHNib3[gUWsyPzd3 NVjLcXk4OjRzN{mxOVI>
THP-1 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XKcFAvODFz4pETPEDPxE1? MkXxPVYhcA>? MnPn[Y5p[W6lZYOgeIhmKGGwdHnwdo9tcW[ncnH0bZZmKGWoZnXjeJMhd2ZiTVuxO|c2 MXOyOFE4QTF3Mh?=
HL-60  NX;pbVJKTnWwY4Tpc44hSXO|YYm= NGf2Z|QyOCCvTR?= MXiwMlUhcA>? NEK0[Yxz\WS3Y3XzJJBpd3OyaH;yfYxifGmxbjDv[kBEcGtzIHH0JJNmemmwZTCzOFU> MnfDNlM6OzR2MUG=
OVCAR-8  MX;GeY5kfGmxbjDBd5NigQ>? NUn5OVU6OSEEtV5CpC=> M37mOFI1KGh? NIPUO5Ni[nKxZ3H0[ZMh[2inbX;0bIVz[XC7LXnu[JVk\WRiY3XscEBkgWOuZTDhdpJme3R? M{XjeVI{PTR6Mk[5
PANC-1 NYHr[nVoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rTTlAvOTFvOTFOwG0> NHn5OXAyKGh? MorxbY5pcWKrdIOgeIhmKGOnbHygeoli[mmuaYT5JIlvKGFiZH;z[U0h\GWyZX7k[Y51KG2jbn7ldi=> MVeyNlgzPTN|MR?=
MiaPaCa NXzjSXhiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkL3NE4yOS17IN88US=> NVTzV442OSCq MnX6bY5pcWKrdIOgeIhmKGOnbHygeoli[mmuaYT5JIlvKGFiZH;z[U0h\GWyZX7k[Y51KG2jbn7ldi=> MnPQNlI5OjV|M{G=
PSN-1 NX\y[Gx6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\IZ2U4OC5zMT25JO69VQ>? MWCxJIg> NVGz[25HcW6qaXLpeJMhfGinIHPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S1iZHXw[Y5l\W62IH3hco5meg>? MlXUNlI5OjV|M{G=

... 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]

+ 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)

  • Mass
    Concentration
    Volume
    Molecular Weight

*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 )

  • C1
    V1
    C2
    V2

* 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

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

ATM/ATR Signaling Pathway Map

ATM/ATR Inhibitors with Unique Features

Related ATM/ATR Products

Tags: buy VE-821 | VE-821 supplier | purchase VE-821 | VE-821 cost | VE-821 manufacturer | order VE-821 | VE-821 distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID