MSA-2-dimer-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEMSA-2dimerCat.No.:HY-141514CASNo.:2377881-92-8分?式:C??H??O?S?分?量:568.66作?靶點(diǎn):STING作?通路:Immunology/Inflammation儲(chǔ)存?式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:70mg/mL(123.10mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.7585mL8.7926mL17.5852mL5mM0.3517mL1.7585mL3.5170mL10mM0.1759mL0.8793mL1.7585mL請(qǐng)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(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)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(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥1.75mg/mL(3.08mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:1.75mg/mL(3.08mM);Suspendedsolution;Needultrasonic1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥1.75mg/mL(3.08mM);ClearsolutionBIOLOGICALACTIVITY?物活性MSA-2dimer?種具有選擇性和?服活性的?核苷酸STING激動(dòng)劑(Kd=145μM)，有長(zhǎng)期抗腫瘤和免疫原活性。MSA-2dimer作為?共價(jià)?聚體與STING結(jié)合，其滲透率?于循環(huán)?核苷酸[1]。IC50&TargetKd:145μM(STING)[1]體內(nèi)研究MSA-2dimer(60mg/kg;p.o.;50days)inhibitstumorgrowthandprolongsoverallsurvival[1].MSA-2dimer(40mg/kg;s.c.;25days)inducescompletetumorregression[1].MSA-2dimer(60mg/kg;p.o.;4hours)increasesproinflammatorycytokine(IFN-β)levelintumors[1].MSA-2dimer(60mg/kg;s.c.;4hours)concentrationsisobservedintumorsthaninplasmaorothernontumortissues[1].MSA-2dimer(THP-1cells)inducesphosphorylationofbothTBK1andIR.MSA-2dimer(10μMand33μM;macrophages)inducesIFN-β[1].MSA-2dimeralsoexhibitsdose-dependentantitumoractivitywhenadministeredbyIT,SC,orPOroutes[1].AnimalModel:B16F10tumor-bearingmiceDosage:60mg/kgAdministration:P.o.;50daysResult:Inhibitedtumorgrowthandprolongedoverallsurvival.AnimalModel:C57BL6miceDosage:40mg/kgAdministration:S.c.;25daysResult:Inducedcompletetumorregression.AnimalModel:C57BL6miceDosage:60mg/kgAdministration:P.o.;4hoursResult:Increasedproinflammatorycytokine(IFN-β)levelintumors.AnimalModel:C57BL6mice2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEDosage:50mg/kgAdministration:S.c.;4hoursResult:MSA-2concentrationswereobservedintumorsthaninplasmaorothernontumortissues.REFERENCES[1].PanBS,etal.Anorallyavailablenon-nucleotideSTINGagonistwithantitumoractivity.Science.2020;369(6506):eaba6098.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedical