ETC-159-ETC-1922159-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEETC-159Cat.No.:HY-18988CASNo.:1638250-96-0Synonyms:ETC-1922159分⼦式:C₁₉H₁₇N₇O₃分⼦量:391.38作⽤靶点:Porcupine;Wnt作⽤通路:StemCell/Wnt储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:50mg/mL(127.75mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.5551mL12.7753mL25.5506mL5mM0.5110mL2.5551mL5.1101mL10mM0.2555mL1.2775mL2.5551mL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%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(6.39mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.39mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性ETC-159(ETC-1922159)有效的，具有⼝服活性的PORCN抑制剂。抑制β-catenin报告因活性的IC50值为2.9nM。IC50&TargetIC50:2.9nM(β-catenin)[1]体外研究ETC-159blocksthesecretionandactivityofallWnts.ETC-159hasrobustactivityinmultiplecancermodelsdrivenbyhighWntsignaling.ETC-159ishighlyefficaciousinmolecularlydefinedcolorectalcancers(CRCs)withR-spondintranslocations[1]体内研究ETC-159inhibitsmousePORCNwithanIC50of18.1nM,whereastheIC50forXenopusPorcnisapproximatelyfourfoldhigher(70nM).ETC-159isremarkablyeffectiveintreatingRSPO-translocationbearingcolorectalcancer(CRC)patient-derivedxenografts.ETC-159exhibitsgoodoralpharmacokineticsinmiceallowingpreclinicalevaluationviaoraladministration.Afterasingleoraldoseof5mg/kg,ETC-159israpidlyabsorbedintothebloodwithaTmaxof~0.5handoralbioavailabilityof100%[1].PROTOCOLCellAssay[1]HEK293cellsstablytransfectedwithSTFreporterandpPGK-WNT3Aplasmid(STF3Acells)aretreatedwithvaryingconcentrationsofcompounds.ForWntsecretion,STF3AcellsaretreatedwithETC-159dilutedin1%fetalbovineserum-containingmedia[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMice:Forhumanxenograftmodels,patient-derivedsolidtissuefragmentsaresubcutaneouslyimplantedinAdministration[1]BALB/cnudemice.Allgroupsarematchedfortumorsizewithequalvariancebeforetreatment.ETC-159formulatedin50%PEG400(vol/vol)inwaterisadministeredbyoralgavageatadosingvolumeof10ꢀμL/gbodyweight[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•SciAdv.2020May22;6(21):eaaz5913.•AmJPhysiolEndocrinolMetab.2021Mar15.•PRACTICALONCOLOGYJOURNAL.2018,32(02):103-106.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].MadanB,etal.WntaddictionofgeneticallydefinedcancersreversedbyPORCNinhibition.Oncogene.2015Aug10.doi:10.1038/onc.2015.280.McePdfHeightCaution:Producthasnotbeenfullyva