UNC5293-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEUNC5293Cat.No.:HY-132200CASNo.:2226789-82-6分?式:C??H??N?O?分?量:518.69作?靶點(diǎn):TAMReceptor;ALK;FLT3作?通路:ProteinTyrosineKinase/RTK儲存?式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(192.79mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.9279mL9.6397mL19.2793mL5mM0.3856mL1.9279mL3.8559mL10mM0.1928mL0.9640mL1.9279mL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(protectfromlight)。-80°C儲存時，請?jiān)?個?內(nèi)使?，-20°C儲存時，請?jiān)?個?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)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(shí)驗(yàn)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(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.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(4.82mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(4.82mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.82mM);ClearsolutionBIOLOGICALACTIVITY?物活性UNC5293?種MERTK選擇性的有效抑制劑(Ki=190pM)。UNC5293抑制MERTK(IC50=0.9nM)，對Axl、Tyro3和Flt3更具選擇性。UNC5293表現(xiàn)出優(yōu)異的??藥代動?學(xué)特性，并可以被?于?髓??病研究。IC50&TargetKi:190pM(MERTK)IC50:0.9nM(MERTK)[1]體外研究UNC5293providesselectivetargetinhibitionincell-basedassays.InculturesofthehumanB-cellacutelymphoblasticleukemia(B-ALL)cellline,UNC5293inhibitsphosphorylationofMERTKwithanIC50of9.4nM.IntheSEMB-ALLcellline,UNC5293islesspotentagainstFLT3,withanIC50of170nM[1].體內(nèi)研究UNC5293(oraladministration;120mg/kg;singledose)effectivelyinhibitMERTKinvivoinorthotopic697B-ALLmicexenografts[1].UNC5293(oralgavage;3mg/kg;singledose)hasexcellentmousePKproperties(7.8hhalf-lifeand58%oralbioavailability),andtheCmaxandAUClastare9.2μMand2.5h*μM,respectively[1].REFERENCES[1].HongchaoZheng,etal.UNC5293,apotent,orallyavailableandhighlyMERTK-selectiveinhibitor.EurJMedChem.2021May17;220:113534.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuse