Bortezomib-PS-341-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEBortezomibCat.No.:HY-10227CASNo.:179324-69-7Synonyms:PS-341;LDP-341;NSC681239分?式:C??H??BN?O?分?量:384.24作?靶點:Proteasome;NF-κB;Apoptosis;Autophagy作?通路:MetabolicEnzyme/Protease;NF-κB;Apoptosis;Autophagy儲存?式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性數(shù)據體外實驗Ethanol:66.67mg/mL(173.51mM;ultrasonicandwarmingandheatto60°C)DMSO:50mg/mL(130.13mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.6025mL13.0127mL26.0254mL5mM0.5205mL2.6025mL5.2051mL10mM0.2603mL1.3013mL2.6025mL請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month(protectfromlight)。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據您的實驗動物和給藥?式選擇適當?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結果的可靠性，澄的儲備液可以根據儲存條件，適當保存；體內實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；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.請依序添加每種溶劑：1%DMSO>>99%saline1/4MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥0.5mg/mL(1.30mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(5.41mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(5.41mM);Clearsolution4.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.41mM);Clearsolution5.請依序添加每種溶劑：10%EtOH>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥4mg/mL(10.41mM);Clearsolution6.請依序添加每種溶劑：10%EtOH>>90%(20%SBE-β-CDinsaline)Solubility:≥4mg/mL(10.41mM);Clearsolution7.請依序添加每種溶劑：10%EtOH>>90%cornoilSolubility:≥4mg/mL(10.41mM);Clearsolution8.請依序添加每種溶劑：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥2.5mg/mL(6.51mM);Clearsolution9.請依序添加每種溶劑：5%DMSO>>95%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.51mM);ClearsolutionBIOLOGICALACTIVITY?物活性Bortezomib(PS-341)?種可逆性和選擇性的蛋?酶體(proteasome)抑制劑，通過靶向蘇氨酸殘有效抑制20S蛋?酶體(Ki=0.6nM)。Bortezomib破壞細胞周期、誘導細胞凋亡以及抑制核因?NF-κB。Bortezomib第?種蛋?酶體抑制劑，具有抗癌活性。IC50&TargetKi:0.6nM(20Sproteasome)[1]體外研究Bortezomib(PS-341)(100nM;8hours)resultsintheaccumulationofcellsinG2-M,withacorrespondingdecreaseinthenumberofcellsinG1[1].Bortezomib(PS-341)(5-100nM;20hours)inducesapoptosisinmantle-celllymphoma(MCL)celllines[3].Bortezomib(PS-341)(20nM;1-14hours)inducesNoxaup-regulationinbothMCLcelllines[3].TheIC50ofBortezomib(PS-341)isfoundtobe2.46nMfor26SproteasomeintheB16F10cells[4].Bortezomib(PS-341)suppressesseveralanti-apoptoticproteins(e.g.,Bcl-XL,Bcl-2,andSTAT-3)[5].CellCycleAnalysis[1]CellLine:PC-3cellsConcentration:100nMIncubationTime:8hoursResult:ResultedintheaccumulationofcellsinG2-M,withacorrespondingdecreaseinthenumberofcellsinG1.ApoptosisAnalysis[3]2/4MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECellLine:JVM-2,Granta-519,Jeko,REC-1cells(MCLcelllines)Concentration:5-100nMIncubationTime:20hoursResult:ThemedianLD50fortheseMCLcelllineswas31nM(range,18.2-60.1nM).WesternBlotAnalysis[3]CellLine:wtp53(Granta-519),mutp53(Jeko)cellsConcentration:20nMIncubationTime:1,2,4,6,14hoursResult:Noxaup-regulationwasdetectedbetween2to4hoursafterbortezomib(PS-341).體內研究Bortezomib(PS-341)(0.3-1mg/kg;i.v.;onceweeklyfor4weeks)inhibitsPC-3TumorGrowthinNudeMice[1].AnimalModel:Malenudemice(xenografttumormodelbearingPC-3cells)[1]Dosage:0.3,1mg/kgAdministration:Intravenousinjection;onceweeklyfor4weeksResult:Resultedinasignificantdecreaseintumorgrowth~60%atdoseof1mg/kg.戶使?本產品發(fā)表的科研?獻?Cell.2019Jul11;178(2):330-345.e22.?NatCancer.2020Feb;1(2):235-248.?NatCommun.2022Oct2;13(1):5789.?NatCommun.2021May11;12(1):2713.?NatCommun.2020Sep4;11(1):4417.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].AdamsJ,etal.Proteasomeinhibitors:anovelclassofpotentandeffectiveantitumoragents.CancerRes.1999Jun1;59(11):2615-22.[2].ShahshahanMA,etal.Potentialusageofproteasomeinhibitorbortezomib(Velcade,PS-341)inthetreatmentofmetastaticmelanoma:basicandclinicalaspects.AmJCancerRes.2011;1(7):913-24.3/4MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE[3].Pérez-GalánP,etal.Theproteasomeinhibitorbortezomibinducesapoptosisinmantle-celllymphomathroughgenerationofROSandNoxaactivationindependentofp53status.Blood.2006Jan1;107(1):257-64.[4].YerlikayaA,etal.CombinedeffectsoftheproteasomeinhibitorbortezomibandHsp70inhibitorsontheB16F10melanomacellline.MolMedRep.2010Mar-Apr;3(2):333-9.[5].MujtabaT,etal.Advancesintheunderstandingofmechanismsandtherapeuticuseofbortezomib.DiscovMed.2011Dec;12(67):471-80.[6].FernándezY,etal.Chemicalblockageoftheproteasomeinhibitoryfunctionofbortezomib:impactontumorcell