ZT-12-037-01-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEZT-12-037-01Cat.No.:HY-122866CASNo.:2328073-61-4分?式:C??H??N?O?分?量:385.5作?靶點:Ras作?通路:GPCR/GProtein儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:8.33mg/mL(21.61mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.5940mL12.9702mL25.9403mL5mM0.5188mL2.5940mL5.1881mL10mM0.2594mL1.2970mL2.5940mL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：50%PEG300>>50%salineSolubility:5mg/mL(12.97mM);Suspendedsolution;Needultrasonic1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性ZT-12-037-01靶向選擇性絲氨酸/蘇氨酸激酶STK19抑制劑，與STK19蛋?具有?親和?相互作?，抑制NRAS驅(qū)動的?素細(xì)胞惡性轉(zhuǎn)化。ZT-12-037-01ATP競爭性抑制劑，可以抑制NRAS的磷酸化，IC50為24nM。體外研究ZT-12-037-01(3μM;14days)significantlyinhibitsmutantNRAS-STK19-drivenmelanocytecolonyformationandproliferation[1].ZT-12-037-01(0-3μM)hasaninhibitoryeffectsofZT-12-037-01onSTK19WTandSTK19D89N-activatedNRASphosphorylationinHPMs[1].CellProliferationAssay[1]CellLine:CDK4(R24C)melanocytecells;hTERTmelanocytecells;p53DDmelanocytecellsConcentration:3μMIncubationTime:14daysResult:Inhibitedmelanocyteproliferation.WesternBlotAnalysis[1]CellLine:STK19WTandSTK19D89NConcentration:0μM,0.1μM,0.3μM,1μM,3μMIncubationTime:Result:InhibitedNRASphosphorylation.體內(nèi)研究ZT-12-037-01(intraperitoneallyinjection;25-50mg/kg;oncedaily;21days)inhibitsgrowthofSK-MEL-2xenograftmelanomaandthesectionsoftumorsindicatesinductionofapoptosisbyincreasingcleavedcaspase-3[1].AnimalModel:SK-MEL-2xenograftmelanomanudemicewithhTERT/p53DD/CDK4(R24C)melanocytes[1]Dosage:25mg/kg;50mg/kgAdministration:Intraperitoneallyinjection;21days;onceadayResult:InhibitedgrowthofSK-MEL-2xenograftmelanoma.REFERENCES[1].YinC,etal.PharmacologicalTargetingofSTK19InhibitsOncogenicNRAS-DrivenMelanomagenesis.Cell.2019Feb21;176(5):1113-2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1127.e16.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forrese