VE-821isaninhibitorofataxiatelangiectasiaandRad3-related(ATR)kinase,achromatin-remodelingproteinthatsensesDNAdamageandactivatestheDNAdamagecheckpointtoinducecellcyclearrest.VE-821exhibitsanticanceractivity,inducingchromosomefragmentation,apoptosis,andcelldeathinvitro.VE-821decreasesphosphorylationofChk1andinducesG2phasecellcyclearrestinpancreaticcancercellsandleukemiacells,sensitizingthemtotheeffectsofrADIation.
| CasNo. | 1232410-49-9 |
|---|---|
| Purity | ≥98% |
| Formula | C18H16N4O3S |
| FormulaWt. | 368.41 |
| IUPACName | 3-Amino-6-[4-(methylsulfonyl)phenyl]-N-phenyl-2-pyrazinecarboxamide |
| Synonym | VE821 |
| Appearance | Lightyellowpowder |
| StoreTemp | -20°C |
|---|---|
| ShipTemp | Ambient |
| InfoSheet | V1600InfoSheetPDF |
|---|
FlynnRL,CoxKE,JeitanyM,etal.AlternativelengtheningoftelomeresrenderscancercellshypersensitivetoATRinhibitors.Science.2015Jan16;347(6219):273-7.PMID:25593184.
VávrováJ,ZárybnickáL,LukášováE,etal.InhibitionofATRkinasewiththeselectiveinhibitorVE-821resultsinradiosensitizationofcellsofpromyelocyticleukaemia(HL-60).RadiatEnvironBiophys.2013Nov;52(4):471-9.PMID:23934411.
PrevoR,FokasE,ReaperPM,etal.ThenovelATRinhibitorVE-821increasessensitivityofpancreaticcancercellstoradiationandchemotherapy.CancerBiolTher.2012Sep;13(11):1072-81.PMID:22825331.
ReaperPM,GriffithsMR,LongJM,etal.SelectivekillingofATM-orp53-deficientcancercellsthroughinhibitionofATR.NatChemBiol.2011Apr13;7(7):428-30.PMID:21490603.
