Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemERalanitentriacetateCat.No.:HY-123875ACASNo.:1637573-04-6Synonyms:EPI-506分?式:C??H??ClO?分?量:521作?靶點(diǎn):AndrogenReceptor作?通路:Others儲(chǔ)存?式:Pureform-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(191.94mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.9194mL9.5969mL19.1939mL5mM0.3839mL1.9194mL3.8388mL10mM0.1919mL0.9597mL1.9194mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:2.5mg/mL(4.80mM);Suspendedsolution;Needultrasonic2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(4.80mM);Suspendedsolution;Needultrasonic3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.80mM);ClearsolutionBIOLOGICALACTIVITY?物活性Ralanitentriacetate(EPI-506)Ralaniten的前藥，?種?創(chuàng)的，具有?服活性的雄激素受體(AR)N端結(jié)構(gòu)域(NTD)抑制劑。Ralanitentriacetate對(duì)全長(zhǎng)和與抗性相關(guān)的AR物種，包括AR-v7都有活性。體外研究Ralanitentriacetate(EPI-506)targetstheN-terminaldomainoftheandrogenreceptor(AR),andisusedformetastaticcastration-resistantprostatecancer(mCRPC)research.EPI-506isafirst-in-class,highly-specificsmallmoleculethatbindstoanoveltargetontheAR,theN-terminaldomain(NTD)anddirectlyinhibitsARtranscriptionalactivitybyblockingtheinteractionoftheARwithtranscriptionalproteins[2].REFERENCES[1].ObstJK,etal.RevealingMetabolicLiabilitiesofRalanitenToEnhanceNovelAndrogenReceptorTargetedTherapies.ACSPharmacolTranslSci.2019;2(6):453-467.Published2019Sep26.[2].Chi,KimNguyenetal.Efficacy,safety,tolerability,andpharmacokineticsofEPI-506(ralanitenacetate),anovelandrogenreceptor(AR)N-terminaldomain(NTD)inhibitor,inmenwithmetastaticcastration-resistantprostatecancer(mCRPC)progressingafterenzalutamideand/orabiraterone.JournalofClinicalOncology35(2017):5032-5032.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresear