RRx-001-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemERRx-001Cat.No.:HY-16438CASNo.:925206-65-1分?式:C?H?BrN?O?分?量:268.02作?靶點:Apoptosis;Parasite作?通路:Apoptosis;Anti-infection儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:≥100mg/mL(373.11mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.7311mL18.6553mL37.3107mL5mM0.7462mL3.7311mL7.4621mL10mM0.3731mL1.8655mL3.7311mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當(dāng)?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(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的?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.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(9.33mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(9.33mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(9.33mM);ClearsolutionBIOLOGICALACTIVITY?物活性RRx-001?種低氧選擇性的表觀遺傳因?，被?作放射或化療敏感劑，能誘發(fā)凋亡，克服?髓瘤的耐藥性。RRx-001具有有效的抗癌活性且毒性極低。RRx-001?個免疫檢查點的抑制劑，可下調(diào)CD47和SIRP-α。RRx-001G6PD的有效抑制劑，具有較強的抗瘧活性。體外研究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.體內(nèi)研究RRx-001(5mg/kgor10mg/kg,I.V.,thrice-weeklyfor24days)inhibitstumorgrowthandprolongssurvivalinaxenograftmousemodel[1].RRx-001(10?mg/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?邊的抑制劑?師www.MedChemEResult:BlockedMMtumorgrowthandenhancessurvival.Treatmentwaswelltolerated,suggestedbynoapparentweightloss.AnimalModel:FemaleBALB/cnudemice(19.2?±?1.7?g)basedonA549lungcancermodel[2].Dosage:10?mg/kg.Administration:IP,twiceaweekandonceaday.Result:Resultedinthemostsignificanttumorgrowthretardation.Reductionofresidentmacrophagesintumor-bearingmiceattenuatestheantitumoractivityofRRx-001.戶使?本產(chǎn)品發(fā)表的科研?獻?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