RBN-2397-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemERBN-2397Cat.No.:HY-136174CASNo.:2381037-82-5分⼦式:C₂₀H₂₃F₆N₇O₃分⼦量:523.43作⽤靶点:PARP作⽤通路:CellCycle/DNADamage;Epigenetics储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:250mg/mL(477.62mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.9105mL9.5524mL19.1048mL5mM0.3821mL1.9105mL3.8210mL10mM0.1910mL0.9552mL1.9105mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存⽅式和期限。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的⼯作液，建议您现⽤现配，当天使⽤；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分⽐指该溶剂在您配制终溶液中的体积占⽐)：1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥4.17mg/mL(7.97mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥4.17mg/mL(7.97mM);ClearsolutionBIOLOGICALACTIVITY1/3MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemE⽣物活性RBN-2397⼀种强效的，跨物种的，且具有⼝服活性的NAD+竞争性PARP7抑制剂，IC50值⼩于3nM。RBN-2397有选择性地结合PARP7(Kd=0.001μM)并可以恢复⼲扰素I型信号转导。RBN-2397有潜⼒⽤于研究晚期或转移性实体肿瘤。IC50&TargetPARP-7PARP-73nM(IC50)1nM(Kd)体外研究RBN-2397(0.0001-100μM;24hours)inhibitscellsproliferationwithanIC50valueof20nMinNCI-H1373lungcancercells[2].RBN-2397(0.4nM-1μM;24hours)showsarestorationoftypeIIFNresponsebyanincreaseinSTAT1phosphorylationasadose-dependentmannerinNCI-H1373humanlungcancercells[2].RBN-2397(0.0001-1μM;24hours)inhibitscellMARylationinacellbiochemialassaywithanEC50valueof1nM[2].CellProliferationAssay[2]CellLine:NCI-H1373lungcancercellsConcentration:0.0001μM;0.001μM;0.001μM;0.1μM;1μM;10μM;100μMIncubationTime:24hoursResult:Blockedcellproliferation.WesternBlotAnalysis[2]CellLine:NCI-H1373lungcancercellsConcentration:0.4nM-1μMIncubationTime:24hoursResult:Increasedp-STAT1proteinexpression.体内研究RBN-2397(oraladministration;3-100mg/kg;oncedaily;24-32days)inducestumor-specificadaptiveimmunememoryinCT26syngeneicmodelwithdurablecompleteresponsesinCT26tumor-bearingBALB/cmice[2].RBN-2397(oraladministration;3-100mg/kg;oncedaily;32days)causescompleteregressionsatthedose100mg/kgandexertsadose-dependenteffectsontumorgrowthatdoselevelsof≥30mg/kg[2].Thehalf-life(t1/2)ofRBN-2397invivois325mins[2].AnimalModel:CB17SCIDmicewithNCI-H1373xenografts[2]Dosage:3mg/kg,10mg/kg,30mg/kg,100mg/kgAdministration:Oraladministration;oncedaily;24-32daysResult:Decreasedtumorvolumeandexertedanti-tumoreffects.REFERENCES2/3MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].RBN-2397-InhibitingPARP7,aKeymonoPARPCancerDependency[2].MelissaVasbinder,etal.RBN-2397:AFirst-in-ClassPARP7InhibitorTargetingaNewlyDiscoveredCancerVulnerabilityinStress-SignalingPathways.McePdfHeightCaution:Producthasnotbeenfullyvalidatedfor