A-770041-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEA-770041Cat.No.:HY-11011CASNo.:869748-10-7分?式:C??H??N?O?分?量:621.73作?靶點:Src作?通路:ProteinTyrosineKinase/RTK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(160.84mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.6084mL8.0421mL16.0842mL5mM0.3217mL1.6084mL3.2168mL10mM0.1608mL0.8042mL1.6084mL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(4.02mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(4.02mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.02mM);ClearsolutionBIOLOGICALACTIVITY?物活性A-770041選擇性的、具有?服活性的Src家族Lck的抑制劑。A-770041抑制Lck，IC50值為147nM在1mMATP的存在下。A-770041對Lck具有?于Fyn300倍的選擇性，F(xiàn)yn另?個參與T細(xì)胞信號傳遞的Src家族激酶。A-770041可?于急性排斥反應(yīng)的研究。IC50&TargetIC50:0.147μM(Lck),9.1μM(Src),14.1μM(Fgr),44.1μM(Fyn)[1]體外研究A-770041selectiveinhibitsLckwithanIC50valueof0.147μM,andinhibitsotherSrcfamilykinaseSrc,Fgr,FynwithIC50sof9.1,14.1and44.1μM,respectively[1].A-770041(0-30μM;2h)dose-dependentlyinhibitsanti-CD3inducedIL-2productionwithanEC50valueof80nM[1].體內(nèi)研究A-770041(2.5mg/kg;i.g.once)inhibitsconcanavalinA-inducedIL-2invivo[1].A-770041(2.5-20mg/kg/day;for14days)dose-dependentlyincreasesthesurvivalratewithdosesof5and10mg/kg/day,andsurvives100%oftransplantedgraftsuntil14dayswithdosesof10and20mg/kg/day[1].AnimalModel:MaleLewisrats[1]Dosage:2.5mg/kgAdministration:Intragastricadministration;2.5mg/kgonceResult:ShowedaninhibitionofconcanavalinA-inducedIL-2withaninvivoEC50valueof78nM.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?ActaPharmacolSin.2021Apr16.?Metabolites.2022,12(9),793.?CellImmunol.2022Jun;376:104531.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].StachlewitzRF,etal.A-770041,anovelandselectivesmall-moleculeinhibitorofLck,preventsheartallograftrejection.JPharmacolExpTher.2005Oct;315(1):36-41.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE[2].AndrewBurchat,etal.DiscoveryofA-770041,asrc-familyselectiveorallyactivelckinhibitorthatpreventsorganallograftrejectionBioorganic&MedicinalChemistryLettersVolume16,Issue1,1January2006,Pages118-122McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedi