Alobresib-GS-5829-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAlobresibCat.No.:HY-109050CASNo.:1637771-14-2Synonyms:GS-5829分⼦式:C₂₆H₂₃N₅O₂分⼦量:437.49作⽤靶点:EpigeneticReaderDomain作⽤通路:Epigenetics储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:83.33mg/mL(190.47mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.2858mL11.4288mL22.8577mL5mM0.4572mL2.2858mL4.5715mL10mM0.2286mL1.1429mL2.2858mL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。-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>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(4.75mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.75mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.75mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Alobresib(GS-5829)⼀种BET溴结构域抑制剂。Alobresib可有效对抗复发且耐药的过表达c-Myc的⼦宫浆液性癌。Alobresib可⽤于转移性去势抵抗性前列腺癌(mCRPC)研究。IC50&TargetBETbromodomain[1]体外研究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.体内研究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.).户使⽤本产品发表的科研⽂献2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师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