TPI-1-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemETPI-1Cat.No.:HY-100463CASNo.:79756-69-7分?式:C??H?Cl?O?分?量:253.08作?靶點(diǎn):Phosphatase作?通路:MetabolicEnzyme/Protease儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:50mg/mL(197.57mM;Needultrasonic)H2O:<0.1mg/mL(ultrasonic;warming;heatto60°C)(insoluble)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM3.9513mL19.7566mL39.5132mL5mM0.7903mL3.9513mL7.9026mL10mM0.3951mL1.9757mL3.9513mL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。-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%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(9.88mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(9.88mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(9.88mM);ClearsolutionBIOLOGICALACTIVITY?物活性TPI-1SHP-1的抑制劑；抑制重組SHP-1的IC50值為40nM。IC50&TargetIC50:40nM(recombinantSHP-1)[1]體外研究SHP-1hasbeenimplicatedasapotentialcancertherapeutictarget.TPI-1iseffectivestartingat10ng/mLinincreasingSHP-1phospho-substratespLck-pY394.TPI-1selectivelyincreasesSHP-1phospho-substrates(pLck-pY394,pZap70andpSlp76)inJurkatTcellsbuthaslittleeffectsonpERK1/2orpLck-pY505.TPI-1inducesmousesplenic-IFNγ+cellsandinducesIFNγ+cellsinhumanperipheralblood[1].體內(nèi)研究TPI-1inhibitsthegrowthofB16melanomatumorsinmiceatatoleratedoraldoseinaTcell-dependentmannerbuthaslittleeffectsonB16cellgrowthinculture.TPI-1thusalsoincreasespLck-pY394andIFNγ+cellsinmice.TPI-1alsoinhibitsB16tumorgrowthandprolongstumormicesurvivalasatolerateds.c.agent[1].PROTOCOLAnimalMice:ForinvivoinductionofpLck-pY394andIFNγ+cellsinmice,C57BL/6JmicearetreatedwithPBSorAdministration[1]TPI-1(1or3mg/kg,s.c.)for4days.Spleensareharvestedonehourpost-treatmentonday4andprocessedintosplenocytes,whichareusedforassessingpLck-pY394levelsbySDS/WesternblottingandforquantificationofIFNγ+cellsbyELISPOTassays.MicearealsotreatedwithTPI-1(10mg/kg,daily,s.c.)toevaluatethetoxicityofthecompoundsinvivo[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?CancerRes.(2022)82(10):1991-2002.?JAllergyClinImmunol.2021Jun15;S0091-6749(21)00936-2.?JNeuroinflammation.2020Mar9;17(1):81.?FrontImmunol.21January2021.?IntImmunopharmacol.2022Jul16;110:109063.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE[1].KunduS,etal.NovelSHP-1inhibitorstyrosinephosphataseinhibitor-1andanalogswithpreclinicalanti-tumoractivitiesastoleratedoralagents.JImmunol.2010Jun1;184(11):6529-36.McePdfHeightCaution:Producthasnotbeenfullyv