Thalidomide-O-amido-C4-NH2-hydrochloride-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEThalidomide-O-amido-C4-NH2hydrochlorideCat.No.:HY-107438ACASNo.:2245697-86-1分?式:C??H??ClN?O?分?量:438.86作?靶點(diǎn):E3LigaseLigand-LinkerConjugates作?通路:PROTAC儲(chǔ)存?式:-20°C,storedundernitrogen,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen,awayfrommoisture)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:250mg/mL(569.66mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.2786mL11.3932mL22.7863mL5mM0.4557mL2.2786mL4.5573mL10mM0.2279mL1.1393mL2.2786mL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(storedundernitrogen,awayfrommoisture)。-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%salineSolubility:≥2.08mg/mL(4.74mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.74mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.74mM);ClearsolutionBIOLOGICALACTIVITY?物活性Thalidomide-O-amido-C4-NH2hydrochloride?種合成的E3連接酶配體-linker偶聯(lián)物，包含于Thalidomide的cereblon配體和1個(gè)linker?？?于合成PROTAC分?[1]。IC50&TargetCereblon體外研究Thalidomide-O-amido-C4-NH2isanamineintermediate(Compound41),whichcanbeusedasisaheterobifunctionalPROTACBETdegrader.Thebromodomainandextra-terminal(BET)familyproteins,consistingofBRD2,BRD3,BRD4,andtestis-specificBRDTmembers,areepigenetic“readers”andplayakeyroleintheregulationofgenetranscription.BETproteinsareconsideredtobeattractivetherapeutictargetsforcancerandotherhumandiseases.Recently,heterobifunctionalsmall-moleculeBETdegradershavebeendesignedbasedupontheproteolysistargetingchimera(PROTAC)concepttoinduceBETproteindegradation[1].Thalidomide-O-amido-C4-NH2isadegron-linker(refertoCompoundDL6-TL).Degron-linker-targetingligand,whereinthelinkeriscovalentlyboundloatleastonedegronandatleastonetargetingligand,thedegronisacompoundcapableofbindingtoanubiquitinligasesuchasanE3ubiquitinligase(eg,cereblon),andthetargetingligandiscapableofbindingtothetargetedprotein(s)[2].REFERENCES[1].ZhouB,etal.DiscoveryofaSmall-MoleculeDegraderofBromodomainandExtra-Terminal(BET)ProteinswithPicomolarCellularPotenciesandCapableofAchievingTumorRegression.JMedChem.2018Jan25;61(2):462-481.[2].JamesBradner,etal.Methodstoinducetargetedproteindegradationthroughbifunctionalmolecules.WO2017024317A2.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedic