Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemENCT-506Cat.No.:HY-112278CASNo.:2231098-99-8分?式:C??H??FN?O?S分?量:478.54作?靶點:AldehydeDehydrogenase(ALDH)作?通路:MetabolicEnzyme/Protease儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:33.33mg/mL(69.65mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.0897mL10.4484mL20.8969mL5mM0.4179mL2.0897mL4.1794mL10mM0.2090mL1.0448mL2.0897mL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%salineSolubility:≥2.5mg/mL(5.22mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.22mM);ClearsolutionBIOLOGICALACTIVITY?物活性NCT-506?種?服?物可利?的醛脫氫酶1A1(ALDH1A1)抑制劑，IC50為7nM[1]。體外研究NCT-506inhibitsALDH1A1,hALDH1A3,hALDH2withIC50sof0.007±0.001,16.4±3.99,and21.5μM,respectively[1].NCT-506(100,10,1,0.1μM,6days)decreasessignificantlycellviabilitywithanEC50of45.6μMinOV-90cells.NCT-506inhibitsMIAPaCa-2,OV-90,andHT-29cellswithIC50sof0.077±0.040,0.161±0.038,and0.048±0.022μMinaldefluorcell-basedassays,respectively[1].NCT-506istreatedincombinedwithPaclitaxel,IC50sof1202,924,870,411,102,and31.8nMwithconcentrationsofNCT-506at0(DMSO),1,3,10,20,30μMinSKOV-3-TRcells,respectively[1].CellViabilityAssay[1]CellLine:OV-90andSKOV-3-TRcellsConcentration:100,10,1,0.1μMIncubationTime:6daysforOV-90cells;4daysforSKOV-3-TRcellsResult:DecreasedsignificantlycellviabilitywithanEC50of45.6μMinOV-90cells.Decreasedcellviabilityincombinedtreatments(Paclitaxelconcentrationof100nM)withanEC50of11.2μMinSKOV-3-TRcells.REFERENCES[1].YangSM,etal.DiscoveryofOrallyBioavailable,Quinoline-BasedAldehydeDehydrogenase1A1(ALDH1A1)InhibitorswithPotentCellularActivity.JMedChem.2018Jun14;61(11):4883-4903.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearc