Polθ-PARP-IN-1-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEPolθ/PARP-IN-1Cat.No.:HY-161302分子式: C₃₈H₃₃ClFN₇O₅S分子量: 754.23作用靶点: Apoptosis;DNA/RNASynthesis;PARP作用通路: Apoptosis;CellCycle/DNADamage;Epigenetics储存方式: PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性Polθ/PARP-IN-1(compound25d)是一种有效的双DNA聚合酶θ(DNApolymerasetheta(Polθ))和PARP抑制剂，IC50值分别为45.6、5.4nM。Polθ/PARP-IN-1显示出抗增殖活性。Polθ/PARP-IN-1诱导细胞凋亡(apoptosis)和细胞周期停滞在G2/M期，导致DNA损伤。Polθ/PARP-IN-1显示出抗肿瘤活性[1]。体外研究Polθ/PARP-IN-1(compound25d)(0-80µM;3days)showsantiproliferativeactivitywithIC50sof20.9,2.7,8.9,2.9,18.9,>80µMforHCC1937,MDA-MB-436,HCT116,SW48,SKOV-3,MCF-10Acells,respectively[1].Polθ/PARP-IN-1(compound25d)(2µM;3days)inducesapoptosisandcellcyclearrestatG2/Mphase,causesDNAdamage[1].CellProliferationAssay[1]CellLine:HCC1937,MDA-MB-436,HCT116,SW48,SKOV-3,MCF-10AcellsConcentration:0-80µMIncubationTime:5daysResult:ShowedantiproliferativeactivitywithIC50sof20.9,2.7,8.9,2.9,18.9,>80µMforHCC1937,MDA-MB-436,HCT116,SW48,SKOV-3,MCF-10Acells,respectively.ApoptosisAnalysis[1]CellLine:MDA-MB-436cellsConcentration:2µM1/2 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEIncubationTime:3daysResult:Inducedapoptosiswithahigherapoptosisrate(26.7%)andarrestedcellcycleprogressionattheG2/Mphase.体内研究Polθ/PARP-IN-1(20,40mg/kg;i.p.;dailyfor21consecutivedays)inhibitstumorgrowthinMDA-MB-436xenograftmodel[1].AnimalModel:18-20g,Six-week-oldfemaleBALB/Cnudemice(MDA-MB-436xenograftmodel)[1]Dosage:20,40mg/kgAdministration:I.p.;dailyfor21consecutivedaysResult:SignificantlyinhibitedthegrowthofMDA-MB-436xenograftsinadose-dependentmanner,exertedanoptimalinhibitorypotencywithatumorgrowthinhibition(TGI)rateof54.4%,74.7%at20,40mg/kg,respectively.REFERENCESMaL,etal.DiscoveryandProofofConceptofPotentDualPolθ/PARPInhibitorsforEfficientTreatmentofHomologousRecombination-DeficientTumors.JMedChem.2024Feb20.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonl