RRx-001-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemERRx-001Cat.No.:HY-16438CASNo.:925206-65-1分⼦式:C₅H₆BrN₃O₅分⼦量:268.02作⽤靶点:Apoptosis;Parasite作⽤通路:Apoptosis;Anti-infection储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥100mg/mL(373.11mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM3.7311mL18.6553mL37.3107mL5mM0.7462mL3.7311mL7.4621mL10mM0.3731mL1.8655mL3.7311mL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。-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.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(9.33mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(9.33mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(9.33mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性RRx-001⼀种低氧选择性的表观遗传因⼦，被⽤作放射或化疗敏感剂，能诱发凋亡，克服⾻髓瘤的耐药性。RRx-001具有有效的抗癌活性且毒性极低。RRx-001⼀个免疫检查点的抑制剂，可下调CD47和SIRP-α。RRx-001G6PD的有效抑制剂，具有较强的抗疟活性。体外研究RRx-001(0-5μM,24hours)inhibitsMMcellsgrowthandovercomesresistancetonovelandconventionaltherapies[1].RRx-001blocksmigrationofMMcellsandassociatedangiogenesis[1].RRx-001inducessignificantG1phasegrowtharrest,withconcomitantdecreaseinSphase.RRx-001triggerssignificantapoptosisinMMcells[1].RRx-001inhibitsDNAmethylationbydownregulatingDNAmethytransferases[1].RRx-001andthesupernatantofRRx-001-treatedmacrophagesdownregulatesCD47ontumorcellsandSIRPαonmacrophages[2].CellViabilityAssay[1]CellLine:HumanMM-celllines(MM.1S,RPMI-8226,H929,ARP1,KMS-11,OPM2,LR5,ANBL6.WT),alongwithdrugresistantcelllinessuchas(MM.1R,Dox40,LR5,ANBL6.BR,RPMI-8226).Concentration:0-5μM.IncubationTime:24hours.Result:Inducedadose-dependentsignificant(p<0.05)decreaseinviabilityofallcelllines.体内研究RRx-001(5mg/kgor10mg/kg,I.V.,thrice-weeklyfor24days)inhibitstumorgrowthandprolongssurvivalinaxenograftmousemodel[1].RRx-001(10ꢀmg/kg,IP,twiceaweekandonceaday)exhibitspotentanti-canceractivityontheA549lungcancermodeldependentonthepresenceoftumor-associatedmacrophages(TAMs)intumortissue[2].AnimalModel:CB-17SCID-miceweresubcutaneouslyinoculatedwith5.0×106MM.1Scellsin100µLofserum-freeRPMI1640medium[1].Dosage:5mg/kgor10mg/kg.Administration:I.V.,thrice-weeklyfor24days.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEResult:BlockedMMtumorgrowthandenhancessurvival.Treatmentwaswelltolerated,suggestedbynoapparentweightloss.AnimalModel:FemaleBALB/cnudemice(19.2ꢀ±ꢀ1.7ꢀg)basedonA549lungcancermodel[2].Dosage:10ꢀmg/kg.Administration:IP,twiceaweekandonceaday.Result:Resultedinthemostsignificanttumorgrowthretardation.Reductionofresidentmacrophagesintumor-bearingmiceattenuatestheantitumoractivityofRRx-001.户使⽤本产品发表的科研⽂献•MolCell.2019Sep19;75(6):1147-1160.e5.•JExpClinCancerRes.2019Feb20;38(1):90.•JMedChem.2022Oct19.•BiomedPharmacother.2021Jun8;111652.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].DasDS,etal.Anovelhypoxia-selectiveepigeneticagentRRx-001triggersapoptosisandovercomesdrugresistanceinmultiplemyelomacells.Leukemia.2016Nov;30(11):2187-2197.[2].CabralesP,etal.RRx-001ActsasaDualSmallMoleculeCheckpointInhibitorbyDownregulatingCD47onCancerCellsandSIRP-αonMonocytes/Macrophages.TranslOncol.2019Apr;12(4):626-632.[3].YalcinO,etal.FromMETStomalaria:RRx-001,amulti-facetedanticanceragentwithactivityincerebralmalaria.MalarJ.2015May28;14:218.McePdfHe