H3B-5942-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEH3B-5942Cat.No.:HY-112611CASNo.:2052128-15-9分⼦式:C₃₁H₃₄N₄O₂分⼦量:494.63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:83.33mg/mL(168.47mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.0217mL10.1086mL20.2171mL5mM0.4043mL2.0217mL4.0434mL10mM0.2022mL1.0109mL2.0217mL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(4.21mM);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(4.21mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性H3B-5942⼀种选择性、不可逆、可⼝服的estrogenreceptor共价拮抗剂，能够靶作⽤于Cys530，使野⽣型和突变型ERα失活，Ki值分别为1nM和0.41nM。H3B-5942能够减少ERα的⽬标因GREB1的表达。H3B-5942具有抗癌作⽤，对含有ERαWT或者突变型ERα的肿瘤细胞和动物具有抗肿瘤活性[1]。IC50&TargetERαY537SERαWT0.41nM(Ki)1nM(Ki)体外研究H3B-5942isaselectiveandirreversibleestrogenreceptorcovalentantagonist,inactivatesbothwild-typeandmutantERαbytargetingCys530,withKisof1nMand0.41nM,respectively[1].H3B-5942elevatesERαproteinleveldistinctfromSERMs/SERD,blocksERα-dependenttranscriptioninbreastcancercells.H3B-5942(0.01-10μM)reducesERαtargetgeneGREB1inMCF7-ERαWT,variousMCF7-ERαMUTlines,andthePDX-ERαY537S/WTline[1].H3B-5942alsodecreasesproliferationofMCF7-Parental,MCF7-LTED-ERαWT,andMCF7-LTED-ERαY537ClineswithGI50sof0.5,2,and30nM,respectively.H3B-5942(10-25nM)incombinationwithCDK4/6inhibitors(≥25pM)hassynergicinhibitoryeffectonmultiplecelllinesbearingERαWTorclinicallyfrequentERαmutations[1].体内研究H3B-5942(1,3,10,or30mg/kg,p.o,q.d.for17days)dose-dependentlyinhibitstumorgrowthinMCF7xenograftmodelinathymicfemalenudemice[1].H3B-5942(3,10,30,100,and200mg/kg,p.o,q.d.)exhibitssimilaranti-tumoractivityintheERαY537S/WTST941modelinathymicfemalenudemice[1].AnimalModel:MCF7xenograftmodelinathymicfemalenudemice[1]Dosage:1,3,10,or30mg/kgAdministration:P.O.onceaday(q.d.×1)for17daysResult:Exhibitedtumorgrowthinhibition(TGI)onday17of19%,41%,68%,and83%,respectively.REFERENCES[1].PuyangX,etal.DiscoveryofSelectiveEstrogenReceptorCovalentAntagonistsfortheTreatmentofERαWTandERαMUTBreastCancer.CancerDiscov.2018Sep;8(9):1176-1193.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedical