NCT-505-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemENCT-505Cat.No.:HY-112277CASNo.:2231079-74-4分?式:C??H??FN?O?S分?量:521.61作?靶點(diǎn):AldehydeDehydrogenase(ALDH)作?通路:MetabolicEnzyme/Protease儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(191.71mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.9171mL9.5857mL19.1714mL5mM0.3834mL1.9171mL3.8343mL10mM0.1917mL0.9586mL1.9171mL請(qǐng)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(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)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(chǔ)備液可以根據(jù)儲(chǔ)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(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(4.79mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.79mM);ClearsolutionBIOLOGICALACTIVITY?物活性NCT-505?種有效的，選擇性的?醛脫氫酶(aldehydedehydrogenase(ALDH1A1))抑制劑，IC50值為7nM，對(duì)hALDH1A2，hALDH1A3，hALDH2，hALDH3A1的抑制作?較弱，IC50值分別為>57，22.8，20.1，>57μM。IC50&TargetIC50:7nM(ALDH1A1),>57μM(hALDH1A2),22.8μM(hALDH1A3),20.1μM(hALDH2),>57μM(hALDH3A1)[1]體外研究NCT-505(Compound86)isapotentandselectivealdehydedehydrogenase(ALDH1A1)inhibitor,withanIC50of7nM,andweaklyinhibitshALDH1A2,hALDH1A3,hALDH2,hALDH3A1(IC50s,>57,22.8,20.1,>57μM).NCT-505hasnoobviousinhibitoryeffecon5-hydroxyprostaglandindehydrogenase(HPGD)andtype-4hydroxysteroiddehydrogenase(HSD17β4)(IC50,>57μM).Moreover,NCT-505showspotentcellularactivities,reducingtheviabilityofOV-90cellswithanEC50of2.10-3.92μM.NCT-505isalsocytotoxictoSKOV-3-TRcells,withIC50sof1,3,10,20,30μM,respectively,inthetitrationassay[1].PROTOCOLCellAssay[1]Cellsareharvested,andanequalvolumeoffirstcompound(NCT-505orpaclitaxel(Taxol))attheindicatedconcentrationorvehicleDMSO(finalDMSOconcentrationisthesameinallconditions)isaddedtothecellsuspensionbeforedispensing.Cellsaredispensedinto384-well,white,TC-treatedplatesatadensityof3000cells/wellinavolumeof30μLofgrowthmedia/wellusingaMultidropCombidispenser.Immediatelyafterdispensing,thesecondcompound(ALDH1A1inhibitororpaclitaxel)andcontrolsolutions(92nL)aretransferredusingapintool.Platesarecoveredwithabreathablesealandincubatedfor4daysat37°C,5%CO2,85%RHfollowedbyadditionof20μLofCellTiter-Glo.Aftera-30minincubationatrt,samplesareanalyzedforluminescenceintensityusingaViewLuxhigh-throughputCCDimagerequippedwithclearfilters.Pinnedcompoundsaretestedas16-pointdilutionseries,withconcentrationsrangingfrom30.7μMto70.1nMforALDH1A1inhibitors(NCT-505,etc.)or31.7μMto0.034nMforpaclitaxel,intriplicate.Dataarenormalizedtopositivecontrolbortezomib(1μMfinal)andneutralcontrolDMSO[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.REFERENCES[1].YangSM,etal.DiscoveryofOrallyBioavailable,Quinoline-BasedAldehydeDehydrogenase1A1(ALDH1A1)InhibitorswithPotentCellularActivity.JMedChem.2018Jun14;61(11):4883-4903.McePdfHeightCaution:Producthasnotbe