ABBV-744-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEABBV-744Cat.No.:HY-112090CASNo.:2138861-99-9分?式:C??H??FN?O?分?量:491.55作?靶點(diǎn):EpigeneticReaderDomain;HIV作?通路:Epigenetics;Anti-infection儲(chǔ)存?式:4°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(203.44mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.0344mL10.1719mL20.3438mL5mM0.4069mL2.0344mL4.0688mL10mM0.2034mL1.0172mL2.0344mL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)。-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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)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:≥2.5mg/mL(5.09mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.09mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.09mM);Clearsolution4.請(qǐng)依序添加每種溶劑：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥2mg/mL(4.07mM);Clearsolution5.請(qǐng)依序添加每種溶劑：5%DMSO>>95%(20%SBE-β-CDinsaline)Solubility:≥2mg/mL(4.07mM);Clearsolution6.請(qǐng)依序添加每種溶劑：50%PEG300>>50%salineSolubility:2.5mg/mL(5.09mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性ABBV-744?種?創(chuàng)，具有?服活性和選擇性的BET家族蛋?BDII結(jié)構(gòu)域(BDIIdomain)，對(duì)BRD2、BRD3、BRD4和BRDT的IC50值為4~18nM。ABBV-744主由CYP3A4代謝，具有類似藥物的特性，可?于研究其抗腫瘤功效和耐受性[1]。IC50&TargetBRD2(BD2)BRD3(BD2)BRDT(BD2)BRD4(BD2)8nM(IC50)13nM(IC50)18nM(IC50)4nM(IC50)BRD4(BD2)3nM(Kd)體外研究ABBV-744(90nM;0~24h;LNCaPcells)downregulatestheexpressionofKLK2andMYCgenes[1].ABBV-744(90nM;0~72h;LNCaPcells)inducescellcyclearrestinG1followedbysenescence[1].WesternBlotAnalysis[1]CellLine:LNCaPcellsConcentration:90nMIncubationTime:0~24hoursResult:DownregulatedtheexpressionofKLK2andMYCgenes.CellCycleAnalysis[1]CellLine:LNCaPcellsConcentration:90nMIncubationTime:0~72hoursResult:InducedcellcyclearrestinG1followedbysenescence.體內(nèi)研究ABBV-744(4.7mg/kg;oralgavage;28days)causesadelayintumorgrowthanddisplaysequivalentorbetterantitumoractivitycomparedwithABBV-075[1].2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEABBV-744(30mg/kg;14days)isabletoproducesignificantantitumoractivity.ABBV-744(30mg/kg)triggersareductioninplateletsofonly20%[1].AnimalModel:MiceDosage:4.7mg/kg(PharmacokineticAnalysis)Administration:Oralgavage;28daysResult:CausedadelayintumorgrowthanddisplayedequivalentorbetterantitumoractivitycomparedwithABBV-075.AnimalModel:Sprague-DawleyratsDosage:30mg/kg(PharmacokineticAnalysis)Administration:14daysResult:Producedsignificantantitumoractivity.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?Cell.2021Apr15;184(8):2167-2182.e22.?Science.2020Apr24;368(6489):387-394.?Analysis&Sensing.22June2022.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].FaivreEJ,etal.SelectiveinhibitionoftheBD2bromodomainofBETproteinsinprostatecancer.Nature.2020;578(7794):306-310.McePdfHeightCaution:Producthasnotbe