Ralaniten-EPI-002-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemERalanitenCat.No.:HY-109070CASNo.:1203490-23-6Synonyms:EPI-002分⼦式:C₂₁H₂₇ClO₅分⼦量:394.89作⽤靶点:AndrogenReceptor作⽤通路:Others储存⽅式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性数据体外实验DMSO:100mg/mL(253.24mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.5324mL12.6618mL25.3235mL5mM0.5065mL2.5324mL5.0647mL10mM0.2532mL1.2662mL2.5324mL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(protectfromlight)。-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>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.33mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性Ralaniten(EPI-002)⼀种有效和具有⼝服活性的雄激素受体N端结构域(AR-NTD)拮抗剂。Ralaniten抑制AR转录活性，IC50值为7.4μM。Ralanites可⽤于去势抵抗性前列腺癌(CRPC)的研究。IC50&TargetIC50:7.4μM(AR-NTD)[1]体外研究EPI-002(5-35μM;2-3days)reducesAR-dependentproliferationofLNCaPcells,andhasnoeffectontheviabilityofPC3humanprostatecancercellsthatdonotexpressfunctionalAR[1].Ralaniten(10-35μM;4h)inhibitstransactivationoftheARN-terminaldomain(NTD)inducedbyforskolininLNCaPcells[1].体内研究EPI-002(100mg/kg;p.o.twicedailyfor28days)inhibitstheVCaPtumorgrowthincastratedmice[1].AnimalModel:MaleNOD-SCIDmicebearingsubcutaneoustumorswerecastratedDosage:100mg/kgAdministration:P.o.twicedailyfor28daysResult:Inhibitedthegrowthofcastration-resistantprostatecancer(CRPC)xenograftsthatexpressARsplicevariants[1].REFERENCES[1].MyungJK,et,al.AnandrogenreceptorN-terminaldomainantagonistfortreatingprostatecancer.JClinInvest.2013Jul;123(7):2948-60.[2].YangYC,et,al.TargetingAndrogenReceptorActivationFunction-1withEPItoOvercomeResistanceMechanismsinCastration-ResistantProstateCancer.ClinCancerRes.2016Sep1;22(17):4466-77.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuse