Forodesine-hydrochloride-BCX-1777-hydrochloride-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEForodesinehydrochlorideCat.No.:HY-16209CASNo.:284490-13-7Synonyms:BCX-1777hydrochloride;Immucillin-Hhydrochloride分?式:C??H??ClN?O?分?量:302.71作?靶點:NucleosideAntimetabolite/Analog;Apoptosis作?通路:CellCycle/DNADamage;Apoptosis儲存?式:-20°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性數(shù)據(jù)體外實驗H2O:100mg/mL(330.35mM;Needultrasonic)DMSO:10mg/mL(33.03mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.3035mL16.5175mL33.0349mL5mM0.6607mL3.3035mL6.6070mL10mM0.3303mL1.6517mL3.3035mL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(storedundernitrogen)。-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：5%DMSO>>40%PEG300>>5%Tween-80>>50%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥0.5mg/mL(1.65mM);Clearsolution2.請依序添加每種溶劑：5%DMSO>>95%(20%SBE-β-CDinsaline)Solubility:≥0.5mg/mL(1.65mM);Clearsolution3.請依序添加每種溶劑：PBSSolubility:36.67mg/mL(121.14mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性Forodesinehydrochloride(BCX-1777hydrochloride)?種?效的?服活性的嘌呤核苷磷酸化酶(PNP)抑制劑，對?，??，??，猴和狗PNP的IC50值在0.48?1.57nM之間。Forodesinehydrochloride有效的?類淋巴細胞增殖抑制劑，可通過增加dGTP?平?誘導(dǎo)??病細胞凋亡(apoptosis)。IC50&TargetIC50:1.19nM(HumanPNP),0.48nM(MousePNP),1.24nM(RatPNP),0.66nM(MonkeyPNP)and1.57nM(DogPNP)[2]體外研究Forodesine(10-30?μM;24and48hours;RPMI-8226,MOLT-4and5T33MMcells)treatmentispartiallyinhibitionofproliferation[1].Forodesine(10-30?μM;24and48hours;RPMI-8226,MOLT-4and5T33MMcells)hasnoeffectontheMMcellsat24hours,whileitcouldreducethepercentageoflivingcellsintheMOLT-4cellswith40%[1].Forodesine(BCX-1777),inthepresenceof2'-deoxyguanosine(dGuo,3-10μM),inhibitshumanlymphocyteproliferationactivatedbyvariousagentssuchasinterleukin-2(IL-2),mixedlymphocytereaction(MLR)andphytohemagglutinin(PHA)(IC50values<0.1-0.38μM)[2].CellProliferationAssay[1]CellLine:HumanRPMI-8226,humanMOLT-4(T-ALL)cells,5T33MM(Multiplemyeloma,MM).Concentration:10?μM,20?μM,30?μMIncubationTime:24and48hoursResult:Attheeffectsat48hours,acompleteblockinproliferationintheMOLT-4cellsand15%reductioninthe5T33MMcells.ApoptosisAnalysis[1]CellLine:HumanRPMI-8226,humanMOLT-4(T-ALL)cells,5T33MM(Multiplemyeloma,MM).Concentration:10?μM,20?μM,30?μMIncubationTime:24and48hoursResult:Alimitedinductionofapoptosis.體內(nèi)研究Forodesine(BCX-1777)hasexcellentoralbioavailability(63%)inmice[2].Atasingledoseof10mg/kginmice,ForodesineelevatesdGuotoapproximately5μM[2].2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEnthehumanperipheralbloodlymphocyteseverecombinedimmunodeficiency(hu-PBL-SCID)mousemodel,Forodesineiseffectiveinprolongingthelifespan2-foldormore[2].戶使?本產(chǎn)品發(fā)表的科研?獻?Cell.2019Oct31;179(4):864-879.e19.?NucleicAcidsRes.2020Sep25;48(17):e101.?NatCommun.2017Aug14;8(1):241.?BiosensBioelectron.2020Dec1;169:112616.?CellRep.2020May12;31(6):107640.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].BieghsL,etal.Theeffectsofforodesineinmurineandhumanmultiplemyelomacells.AdvHematol.2010;2010:131895.[2].BantiaS,etal.PurinenucleosidephosphorylaseinhibitorBCX-1777(Immucillin-H)--anovelpotentandorallyactiveimmunosuppressiveagent.IntImmunopharmacol.2001Jun;1(6):1199-210.McePdfHeightCautio