Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPARP1-IN-5dihydrochlorideCat.No.:HY-132297A分?式:C??H??Cl?N?O?S分?量:537.46作?靶點(diǎn):PARP作?通路:CellCycle/DNADamage;Epigenetics儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:125mg/mL(232.58mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.8606mL9.3030mL18.6060mL5mM0.3721mL1.8606mL3.7212mL10mM0.1861mL0.9303mL1.8606mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(3.87mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(3.87mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.87mM);ClearsolutionBIOLOGICALACTIVITY?物活性PARP1-IN-5dihydrochloride?種低毒、具有?服活性、有效的和有選擇性的PARP-1抑制劑(IC50=14.7nM)。PARP1-IN-5dihydrochloride可?于癌癥研究[1]。IC50&TargetPARP-1PARP-214.7nM(IC50)0.9μM(IC50)體外研究PARP1-IN-5dihydrochloride(0.1~10μM;A549cells)cansignificantlyincreasethecytotoxicityofCBPonA549cellsinadose-dependentmanner.PARP1-IN-5dihydrochloride(0.1~10μM;SK-OV-3cells)decreasestheexpressionsofMCM2-7.PARP1-IN-5dihydrochloride(0.1~320μM;A549cells)haslittlecytotoxiceffectsonA549cells.PARP1-IN-5dihydrochloride(SK-OV-3cells)cansignificantlydecreasethePARlevel[1].PARP1-IN-5dihydrochlorideexertsantitumoreffectsthroughPARP-1.PARP1-IN-5dihydrochloridecouldincreasetheγ-H2AXexpression[1].體內(nèi)研究PARP1-IN-5dihydrochloride(1000mg/kg;p.o.)showsthatthereisnosignificantdifferenceinthebodyweightandbloodroutine[1].PARP1-IN-5dihydrochloride(25and50mg/kg;p.o.;12days)significantlyenhancestheinhibitoryeffectofcarboplatinonA549cellsat50mg/kg[1].PARP1-IN-5dihydrochloride(50mg/kg;p.o.)positivelycorrelateswiththeexpressionofPARP-1[1].PARP1-IN-5dihydrochloridecanupregulatetheexpressionofγ-H2AXanddecreasetheexpressionofPAR[1].AnimalModel:Mice[1]Dosage:1000mg/kgAdministration:P.o.Result:Therewasnosignificantdifferenceinthebodyweightandbloodroutine.AnimalModel:Mice[1]Dosage:25and50mg/kgAdministration:P.o.;12daysResult:SignificantlyenhancedtheinhibitoryeffectofCBPonA549cellsat50mg/kg.AnimalModel:MaleSprague?Dawley(SD)rats[1]2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEDosage:50mg/kg(PharmacokineticAnalysis)Administration:P.o.Result:PositivelycorrelatedwiththeexpressionofPARP-1.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?Apoptosis.2022Feb4.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].LongH,etal.DiscoveryofNovelApigenin-PiperazineHybridsasPotentandSelectivePoly(ADP-Ribose)Polymerase-1(PARP-1)InhibitorsfortheTreatmentofCancer.JMedChem.2021;64(16):12089-12108.McePdfHeightCaution:Producthasnotbeenfully