H3B-6545-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEH3B-6545Cat.No.:HY-112596CASNo.:2052130-80-8分⼦式:C₃₀H₂₉F₄N₅O₂分⼦量:567.58作⽤靶点:EstrogenReceptor/ERR作⽤通路:Others储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:250mg/mL(440.47mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.7619mL8.8093mL17.6187mL5mM0.3524mL1.7619mL3.5237mL10mM0.1762mL0.8809mL1.7619mL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:≥2.08mg/mL(3.66mM);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:≥2.08mg/mL(3.66mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性H3B-6545⼀种有效的，具有⼝服活性的选择性雌激素受体共价拮抗剂(SERCA)。H3B-6545可⽤于研究转移性ER阳性，HER2性乳腺癌[1][2]。IC50&TargetEstrogenreceptor[1]体外研究H3B-6545isahighlyselectivesmallmoleculethatpotentlyantagonizeswild-typeandmutantERαinbiochemicalandcellbasedassays.InvitrocomparisonswithstandardofcareandotherexperimentalagentsconfirmincreasedcellpotencyofH3B-6545undercontinuousaswellaswashouttreatmentconditions[1].H3B-6545,amemberofanovelclassofERαantagonistsrefertoasselectiveERcovalentantagonist(SERCA),whichinactivatesbothwild-typeandmutantERαbytargetingC530andenforcingauniqueantagonistconformation.H3B-6545isafirst-in-classselectiveERcovalentantagonist(SERCA).H3B-6545inhibitsERαWTactivityandgrowthofERαWT-positivebreastcancerlines.H3B-6545potentlyinhibitsERαWTactivityandsuppressesproliferationofERαWT-positivebreastcancerlines.WithGI50sof0.3-0.4,1.0,0.5,5.2,and0.2nMforMCF7,HCC1428,BT483,T47DandCAMA-1celllines[1].体内研究Invivo,oncedailyoraldosingofH3B-6545showspotentactivityandsuperiorefficacytofulvestrantintheMCF-7xenograftmodelwithmaximalantitumoractivityatdoses>10xbelowthemaximumtolerateddoseinmice.Inaddition,H3B-6545showssuperiorantitumoractivitytoTamoxifenandFulvestrantinpatientderivedxenograftmodelsofestrogenreceptorpositivebreastcancerincludingmodelscarryingERαmutationsinratandmonkeys,H3B-6545iswelltoleratedacrossabroaddoserangeandatexposuresthatsignificantlyexceedthoserequiredforefficacyinmousexenograftmodels[1].户使⽤本产品发表的科研⽂献•BiolTraceElemRes.2020Feb;34(2):e4746.•JPharmBiomedAnal.2019Aug5;172:189-199.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].PeterG.Smith,etal.AbstractDDT01-04:DiscoveryanddevelopmentofH3B-6545:Anovel,oral,selectiveestrogenreceptorcovalentantagonist(SERCA)forthetreatmentofbreastcancer.AACRAnnualMeeting2017;April1-5.[2].AmyHKim,etal.H3B-6545,aselectiveestrogenreceptorcovalentantagonist,preventsbonelossinovariectomizedSprague-Dawleyrats.JPharmacolToxicolMethods.Sep-Oct2019;99:106595.McePdfHeightCaution:Producthasnotbeenful