Verteporfin-CL-318952-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEVerteporfinCat.No.:HY-B0146CASNo.:129497-78-5Synonyms:CL318952分⼦式:C₄₁H₄₂N₄O₈分⼦量:718.79作⽤靶点:YAP;Apoptosis;Autophagy作⽤通路:StemCell/Wnt;Apoptosis;Autophagy储存⽅式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性数据体外实验DMSO:≥200mg/mL(278.25mM)DMF:10mg/mL(13.91mM;ultrasonicandwarmingandheatto60°C)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM1.3912mL6.9561mL13.9123mL5mM0.2782mL1.3912mL2.7825mL10mM0.1391mL0.6956mL1.3912mL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；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month(protectfromlight)。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。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。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：10%DMF>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(3.48mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥5mg/mL(6.96mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥5mg/mL(6.96mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Verteporfin(CL318952)⼀种⽤于光动⼒疗法的光敏剂，⽤于消除与年龄相关的斑变性等疾病相关的眼内异常⾎管。Verteporfin⼀种YAP抑制剂，可破坏YAP-TEAD相互作⽤。Verteporfin可以诱导细胞凋亡(apoptosis)。Verteporfin⼀种⾃噬(autophagy)抑制剂，通过抑制⾃噬⼩体形成，在早期阻断⾃噬。IC50&TargetIC50:YAP-TEADinteraction体外研究VerteporfinisspecificallyselectedbyPDX-cellscreening.Theconcentrationstocause50%growthinhibition(GI50)forPhLO,PhLH,andPhLKare228nM,395nM,and538nM,respectively,whereasGI50forALL-1,TCC-Y/sr,andNPhA1are3.93µM,2.11µM,and5.61µM,respectively.GSHsignificantlyreducesthesensitivityof2outof3PDXcellstoverteporfin.VerteporfinreducesthemitochondrialmembranepotentialinPDXcells[1].VerteporfinreducesthePTX-resistanceonHCT-8/TcellsbyinhibitingYAPexpressionandcombinationtherapywithverteporfinandNSC125973showssynergismoninhibitionofYAPandcytotoxicitytoHCT-8/T[2].体内研究Verteporfin(10mg/kg,c.s.c.)andBMS-354825significantlyreducestheleukemiacellratio,andcombinedtherapyfurtherreducedthenumberofleukemiacellsinthespleen[1].PROTOCOLCellAssay[1]PDXcellsco-culturedwithS17cellsaretreatedwith16combinationsofverteporfin(60nM,120nM,180nM,and240nM)andBMS-354825(12nM,24nM,36nM,and48nM).Theviabilitiesofcellstreatedwitheachcombinationaremeasuredafter48husingFACSAriaflowcytometer.InordertoestimatedruginteractionbetweenverteporfinandBMS-354825,anormalizedisobologramandfractionaffectedcombinationindex(CI)plotaremadeusingCompuSynsoftware.CIvaluesgreaterthan1.0indicatedantagonisticeffects,equalto1.0additiveeffects,andbelow1.0synergisticeffects.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMice:PhLOcells(1.0×107/mouse)areinjectedintravenouslyinto6-week-oldmaleNOGmice,whichareAdministration[1]thentreatedwithvehicle,verteporfin(140mg/kg/day),BMS-354825(20mg/kg/day),andacombinationofthesedrugsfromdays22to28.Verteporfinisadministeredbycontinuoussubcutaneousinfusion(c.s.c.)usingAlzetosmoticpumps.Anintraperitonealinjection(i.p.)isperformedforBMS-354825.Allmicearesacrificedonday28andthechimerismofleukemiacellsisinvestigatedbyflowcytometerusingananti-humanCD19antibodyandantimouseCD45antibody.Bloodconcentrationsofverteporfinarecalculatedby2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemELCMS-2020.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•CellRes.2022Jun;32(6):543-554.•CellRes.2020Mar;30(3):229-243.•CancerCell.2019Sep16;36(3):302-318.e7.•NatNeurosci.2022Jul;25(7):849-864.•SciBull.2021May15;66(9):925-936.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].MorishitaT,etal.Thephotosensitizerverteporfinhaslight-independentanti-leukemicactivityforPh-positiveacutelymphoblasticleukemiaandsynergisticallyworkswithBMS-354825.Oncotarget.2016Aug2.[2].PanW,etal.VerteporfincanReversetheNSC125973ResistanceInducedbyYAPOver-ExpressioninHCT-8/TCellswithoutPhotoactivationthroughInhibitingYAPExpression.CellPhysiolBiochem.2016;39(2):481-90.[3].DonohueE,etal.Theautophagyinhibitorverteporfinmoderatelyenhancestheantitumoractivityofgemcitabineinapancreaticductaladenocarcinomamodel.J