LLY-283-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemELLY-283Cat.No.:HY-107777CASNo.:2040291-27-6分?式:C??H??N?O?分?量:342.35作?靶點(diǎn):HistoneMethyltransferase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:125mg/mL(365.12mM;Needultrasonic)H2O:3.57mg/mL(10.43mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.9210mL14.6049mL29.2099mL5mM0.5842mL2.9210mL5.8420mL10mM0.2921mL1.4605mL2.9210mL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%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.08mg/mL(6.08mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(6.08mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(6.08mM);ClearsolutionBIOLOGICALACTIVITY?物活性LLY-283?種有效的，選擇性的，可?服的蛋?精氨酸甲轉(zhuǎn)移酶5(PRMT5)抑制劑，對(duì)PRMT5:MEP50復(fù)合物的作?很強(qiáng)，IC50和Kd值分別為22nM和6nM，具有抗腫瘤活性。IC50&TargetIC50:22nM(PRMT5:MEP50)[1]Ki:6nM(PRMT5:MEP50)[1]體外研究LLY-283isapotent,oralandselectiveargininemethyltransferase5(PRMT5)inhibitor,withanIC50of22nMinvitroand25nMincells,aswellasaKdof6nMforPRMT5:MEP50complexinvitro;LLY-283inhibitstheproliferationofA375cellwithanIC50of46nM[1].體內(nèi)研究LLY-283(20mg/kg;p.o.,QD(onceaday))causesasignificantinhibitionontumorgrowthinmicebearingA375cellsaftertreatmentfor28days[1].戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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