LLY-283-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemELLY-283Cat.No.:HY-107777CASNo.:2040291-27-6分⼦式:C₁₇H₁₈N₄O₄分⼦量:342.35作⽤靶点:HistoneMethyltransferase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:125mg/mL(365.12mM;Needultrasonic)H2O:3.57mg/mL(10.43mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.9210mL14.6049mL29.2099mL5mM0.5842mL2.9210mL5.8420mL10mM0.2921mL1.4605mL2.9210mL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%saline1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(6.08mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(6.08mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(6.08mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性LLY-283⼀种有效的，选择性的，可⼝服的蛋⽩精氨酸甲转移酶5(PRMT5)抑制剂，对PRMT5:MEP50复合物的作⽤很强，IC50和Kd值分别为22nM和6nM，具有抗肿瘤活性。IC50&TargetIC50:22nM(PRMT5:MEP50)[1]Ki:6nM(PRMT5:MEP50)[1]体外研究LLY-283isapotent,oralandselectiveargininemethyltransferase5(PRMT5)inhibitor,withanIC50of22nMinvitroand25nMincells,aswellasaKdof6nMforPRMT5:MEP50complexinvitro;LLY-283inhibitstheproliferationofA375cellwithanIC50of46nM[1].体内研究LLY-283(20mg/kg;p.o.,QD(onceaday))causesasignificantinhibitionontumorgrowthinmicebearingA375cellsaftertreatmentfor28days[1].户使⽤本产品发表的科研⽂献•NeurosciLett.2022Mar9;136576.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].ZahidQ.Bonday,etal.LLY-283,aPotentandSelectiveInhibitorofArginineMethyltransferase5,PRMT5,withAntitumorActivity.ACSMed.Chem.Lett.,2018,9(7),pp612-617.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseon