VE-821

Catalog No.S8007

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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VE-821 Chemical Structure

VE-821 Chemical Structure
Molecular Weight: 368.41

Validation & Quality Control

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Quality Control & MSDS

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Product Information

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Product Description

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)
IC50 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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
U2OS M4LSbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NGrrXYVKSzVy784eNE45KM7:TR?=MXuyOVU6OzF6NB?=
SAOS2MlzNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M3\4OWlEPTExv[6wMlgh|ryPNW\RRWNJOjV3OUOxPFQ>
CAL72NEHM[YhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NIr1S5NKSzVy784eNE45KM7:TR?=M3rIXFI2PTl|MUi0
NOS1MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MV\JR|Ux973gMD64JO69VQ>?NXHW[GVtOjV3OUOxPFQ>
HUO9MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?Mk\STWM2OO,;nkCuPEDPxE1?MoPqNlU2QTNzOES=
MG63MnPFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NEf3ZmdKSzVy784ePUDPxE1?NYD5WXZVOjV3OUOxPFQ>
SJSA1MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MnLpTWM2OO,;nkmg{txOMWiyOVU6OzF6NB?=
MDA-MB-231MXnDfZRwfG:6aXPpeJkhSXO|YYm=M3vVW|EwOy9zMDFOwG0>M1:0ZlEhcA>?NFPrfGVxd3SnboTpZZRmeyC2aHWgZ5l1d3SxeHnjbZR6KG:oIHLveIgh[2GvcITveIhm[2mwIHHu[EBNVVBvNECwMWCyOVI3QTR5OR?=
HT-29M{[2ZWN6fG:2b4jpZ4l1gSCDc4PhfS=>MmHYNU8{NzFyIN88US=>NHPwd|EyKGh?NYLpfFJJeG:2ZX70bYF1\XNidHjlJIN6fG:2b4jpZ4l1gSCxZjDic5RpKGOjbYD0c5Rp\WOrbjDhcoQhVE2SLUSwNC=>Ml3rNlUzPjl2N{m=
HCT-116 p53+/+NWPWR2l4S3m2b4TvfIlkcXS7IFHzd4F6MnX0NU8{NzFyIN88US=>NIPEfWEyKGh?M{HJd5BwfGWwdHnheIV{KHSqZTDjfZRwfG:6aXPpeJkhd2ZiYn;0bEBk[W2ydH;0bIVkcW5iYX7kJGxOWC12MEC=Mm\rNlUzPjl2N{m=
HCT-116 p53-/-MX\DfZRwfG:6aXPpeJkhSXO|YYm=MoW0NU8{NzFyIN88US=>M2D5VlEhcA>?M1\RWpBwfGWwdHnheIV{KHSqZTDjfZRwfG:6aXPpeJkhd2ZiYn;0bEBk[W2ydH;0bIVkcW5iYX7kJGxOWC12MEC=NXHDUFVzOjV{Nkm0O|k>
TF-1MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NHSzNGgxNjBzMfMAl|gh|ryPM3HGdlk3KGh?NV76VnhU\W6qYX7j[ZMhfGinIHHueIlxem:uaX\ldoF1cX[nIHXm[oVkfHNib3[gUWsyPzd3NIfLT28zPDF5OUG1Ni=>
HELMWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NUX6OVhSOC5yMUJihLM5KM7:TR?=NVvXVJQ6QTZiaB?=MVPlcohidmOnczD0bIUh[W62aYDyc4xq\mW{YYTpeoUh\W[oZXP0d{Bw\iCPS{G3O|U>M4fjdVI1OTd7MUWy
THP-1M3LPUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NX\tZ5ZbOC5yMUJihLM5KM7:TR?=M2jr[Vk3KGh?NUfVS4tr\W6qYX7j[ZMhfGinIHHueIlxem:uaX\ldoF1cX[nIHXm[oVkfHNib3[gUWsyPzd3MX2yOFE4QTF3Mh?=
HL-60 NFzwPIdHfW6ldHnvckBCe3OjeR?=M{LjSVExKG2PM3L6fFAvPSCqNUn2OY5PemWmdXPld{BxcG:|cHjvdplt[XSrb36gc4YhS2itMTDheEB{\XKrbnWgN|Q2NInJPGQzOzl|NESxNS=>
OVCAR-8 MmnMSpVv[3Srb36gRZN{[Xl?NID4[lcyKML3TdMgMoH1NlQhcA>?MXjhZpJw\2G2ZYOgZ4hmdW:2aHXyZZB6NWmwZIXj[YQh[2WubDDjfYNt\SCjcoLld5Q>MluxNlM2PDh{Nkm=
PANC-1MonCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M1XU[lAvOTFvOTFOwG0>MlzYNUBpNX;sZo5NcW6qaXLpeJMhfGinIHPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S1iZHXw[Y5l\W62IH3hco5meg>?NILMbFIzOjh{NUOzNS=>
MiaPaCaNYrwc2JYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=Mo\VNE4yOS17IN88US=>MYexJIg>NUTaTlIxcW6qaXLpeJMhfGinIHPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S1iZHXw[Y5l\W62IH3hco5meg>?NYHlVFhXOjJ6MkWzN|E>
PSN-1Mn7IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NUTUTmR{OC5zMT25JO69VQ>?NF:5XZYyKGh?NV;KWIJjcW6qaXLpeJMhfGinIHPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S1iZHXw[Y5l\W62IH3hco5meg>?M4O2cVIzQDJ3M{Ox

... Click to View More Cell Line Experimental Data

In vivo
Features

Protocol(Only for Reference)

Kinase Assay: [2]

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's instructions, and washed six times with 200 μL of 100 mM phosphoric acid, prior to the addition of 100 μL of scintillation cocktail and scintillation counting on a 1450 Microbeta Liquid Scintillation Counter. Dose−response data are analyzed using GraphPad Prism software

Cell Assay: [2]

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Reaper PM, et al. Nat Chem Biol, 2011, 7(7), 428-430.

[2] Charrier JD, et al. J Med Chem, 2011, 54(7), 2320-2330.

Chemical Information

Download VE-821 SDF
Molecular Weight (MW) 368.41
Formula

C18H16N4O3S

CAS No. 1232410-49-9
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 74 mg/mL (200.86 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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 Name 2-Pyrazinecarboxamide, 3-amino-6-[4-(methylsulfonyl)phenyl]-N-phenyl-

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.

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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