NCT-506-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemENCT-506Cat.No.:HY-112278CASNo.:2231098-99-8分⼦式:C₂₅H₂₃FN₄O₃S分⼦量:478.54作⽤靶点:AldehydeDehydrogenase(ALDH)作⽤通路:MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:33.33mg/mL(69.65mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.0897mL10.4484mL20.8969mL5mM0.4179mL2.0897mL4.1794mL10mM0.2090mL1.0448mL2.0897mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(5.22mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.22mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性NCT-506⼀种⼝服⽣物可利⽤的醛脱氢酶1A1(ALDH1A1)抑制剂，IC50为7nM[1]。体外研究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