Estrogen-receptor-modulator-10-DataSheet-生命科學試劑-MCE

Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemEEstrogenreceptormodulator10Cat.No.:HY-155406CASNo.:2991504-90-4分子式:C??H??F?N?O?S分子量:728.71作用靶點:EstrogenReceptor/ERR;Caspase;Bcl-2Family作用通路:VitaminDRelated/NuclearReceptor;Apoptosis儲存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性Estrogenreceptormodulator10(compoundG-5b)是雌激素受體(ER)拮抗劑(IC50=6.7nM)和降解劑(DC50=0.4nM)。Estrogenreceptormodulator10可以通過蛋白酶體途徑迅速降解。Estrogenreceptormodulator10可以誘導細胞凋亡。Estrogenreceptormodulator10可以把細胞阻滯在G1/G0期。Estrogenreceptormodulator10能夠用于癌癥的研究[1]。IC50&TargetIC50=6.7nM,DC50=0.4nM體外研究Estrogenreceptormodulator10(20-100nM,2-48h)significantlyreducesERactivityinT47Dcellsinadose-dependentmanner,anddegradesERinMCF-7cellslaterthaninT47Dcells[1].Estrogenreceptormodulator10(10nM,24h)canreducethegrowthregulationofTFF-1(trefoilfactor1),PgR(progesteronereceptor)andGRBE1(GRBE1)producedbyE2stimulationinMCF-7andT47Dcellsbyestrogeninbreastcancer1)[1].Estrogenreceptormodulator10(4-100nM,24h)inducesapoptosisinMCF-7cells,andsignificantlyenhancestheactivityofcaspase-3andcaspase-9inMCF-7cells[1].Estrogenreceptormodulator10(4-100nM,24h)caninhibittheexpressionofG1/G0phaseproteininMCF-7cells[1].Estrogenreceptormodulator10(0.2-1nM,6d)significantlyinhibitstheproliferationofMCF-7andT47DcellsmediatedbyE2[1].Estrogenreceptormodulator10(4-100nM,24h)significantlyreducesthelevelsofcellmigrationandproliferatingnuclearantigeninMCF-7cells[1].Estrogenreceptormodulator10(20-100nM,24h)reducesERincytoplasmandnucleusinMCF-7cells,promotingthetransferofERfromnucleustocytoplasm.ERisrapidlydegradedthroughproteasomepathwaywithoutaffectingtheexpressionofcorrespondingmRNA[1].1/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemECellViabilityAssay[1]CellLine:T47D,MCF-7Concentration:100nMIncubationTime:24hResult:SignificantlydecreasedtheactivityofERinadose-dependentmanner.RT-PCR[1]CellLine:T47D,MCF-7Concentration:10nMIncubationTime:24hResult:HadantagonisticactivityagainstERsignaling.CellCycleAnalysis[1]CellLine:MCF-7Concentration:4nM,20nM,100nMIncubationTime:24hResult:BlockedcellsintheG1/G0phasewithadose-dependentmanner.CellProliferationAssay[1]CellLine:T47D,MCF-7Concentration:0.2nMforMCF-7cells1nMforT47DcellsIncubationTime:6dResult:CouldselectivelyinhibittheproliferationandmigrationofER-positivebreastcancercellswithoutaffectingER-negativeones.CellProliferationAssay[1]CellLine:T74DWT,T74DY537S,T74DD538GConcentration:2.21nMforT74DWT5.94nMforT74DY537S58.57nMforT74DD538GIncubationTime:5dResult:Inhibitedmutantcellproliferationinadose-dependentmanner.2/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemE體內研究Estrogenreceptormodulator10(30mg/kgIntramuscularinjection(i.m.),singledose)showsfavorablepharmacokineticpropertiesinfemaleSprague-Dawleymice[1].AnimalModel:FemaleSprague-DawleyRats[1]Dosage:30mg/kgAdministration:Intramuscularinjection(i.m.),singledoseResult:Showedapparentdistributionvolume(Vz_F_obs≈1600L)wasnearly1.3timessmallerthanthatoffulvestrant(Vz_F_obs≈2100L),andmostdrugscouldbewidelydistributedfrombloodtotargettissuesandorgans.REFERENCESBingsiWang,etal.Anovelscaffoldlong-actingselectiveestrogenreceptorantagonistanddegraderwithsuperiorpreclinicalprofileagainstER+breastcancer,EuropeanJournalofMedicinalChemistry,2023.McePdfHeightCaution:Prod