Alobresib-GS-5829-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEAlobresibCat.No.:HY-109050CASNo.:1637771-14-2Synonyms:GS-5829分?式:C??H??N?O?分?量:437.49作?靶點(diǎn):EpigeneticReaderDomain作?通路:Epigenetics儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:83.33mg/mL(190.47mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.2858mL11.4288mL22.8577mL5mM0.4572mL2.2858mL4.5715mL10mM0.2286mL1.1429mL2.2858mL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(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%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.08mg/mL(4.75mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.75mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.75mM);ClearsolutionBIOLOGICALACTIVITY?物活性Alobresib(GS-5829)?種BET溴結(jié)構(gòu)域抑制劑。Alobresib可有效對(duì)抗復(fù)發(fā)且耐藥的過(guò)表達(dá)c-Myc的?宮漿液性癌。Alobresib可?于轉(zhuǎn)移性去勢(shì)抵抗性前列腺癌(mCRPC)研究。IC50&TargetBETbromodomain[1]體外研究Alobresib(0.1nM-100μM;72hours)inhibitscellproliferationinprimaryuterineserouscarcinoma(USC)lines[1].CellProliferationAssay[1]CellLine:Primaryuterineserouscarcinoma(USC)linesARK1andARK2celllinesConcentration:0.1nM,10nM,1μM,100μMIncubationTime:72hoursResult:Aprogressive,doseresponsedecreaseincellproliferation.IC50sof27nMand31nMforARK2andARK1cells,respectively.體內(nèi)研究Alobresib(10and20mg/kg;oral;twice-daily;for28days)impairesUSC-ARK2xenografttumorgrowthinfemaleCB17/lcrHsd-Prkd/scidmice.Alobresibexhibitsasignificantlyslowerrateoftumorgrowthinmice,comparedwithvehiclecontrolandtomiceundergoingdailytreatmentwithJQ1(50mg/kg/dayi.p.)[1].Alobresib(10and20mg/kg;oral;twice-daily;for28days)iswelltoleratedwithnoclearimpactonbodyweightcomparedwithvehiclecontrol[1].AnimalModel:FemaleCB17/lcrHsd-Prkd/scidmice(15-19g)bearingUSC-ARK2tumors[1]Dosage:10and20mg/kgAdministration:Oral;twice-daily;28daysResult:Exhibitedasignificantlyslowerrateoftumorgrowth,comparedwithvehiclecontrolandtomiceundergoingdailytreatmentwithJQ1(50mg/kg/dayi.p.).戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE?Cell.2021Apr15;184(8):2167-2182.e22.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].RahulAggarwal,etal.PhaseIbStudyoftheBETInhibitorGS-5829asMonotherapyandCombinedwithEnzalutamideinPatientswithMetastaticCastration-ResistantProstateCancer.ClinCancerRes.2022Sep15;28(18):3979-3989.[2].BonazzoliE,etal.InhibitionofBETBromodomainProteinswithGS-5829andGS-626510inUterineSerousCarcinoma,aBiologicallyAggressiveVariantofEndometrialCancer.ClinCancerRes.2018Oct1;24(19):4845-4853.McePdfHeightCaution:Producthasnotbeenfullyval