EPZ031686-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEEPZ031686Cat.No.:HY-19324CASNo.:1808011-22-4分⼦式:C₂₆H₃₄ClF₃N₄O₄S分⼦量:591.09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:35mg/mL(59.21mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.6918mL8.4589mL16.9179mL5mM0.3384mL1.6918mL3.3836mL10mM0.1692mL0.8459mL1.6918mL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%salineSolubility:≥1.75mg/mL(2.96mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥1.75mg/mL(2.96mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥1.75mg/mL(2.96mM);Clearsolution4.请依序添加每种溶剂：30%PEG300>>70%(20%SBE-β-CDinsaline)Solubility:10mg/mL(16.92mM);Suspendedsolution;NeedultrasonicandwarmingBIOLOGICALACTIVITY⽣物EPZ031686⼀种有效的⼝服活性SMYD3抑制剂，其IC50值为3nM。EPZ031686可⽤于癌症研究。活性IC50&SMYD3Target3nM(IC50)体内研EPZ031686(1-50mg/mL;p.o.andi.v.;MaleCD-1mice)hasgoodbioavailabilityfollowingoraldosinginmice[1].究AnimalModel:MaleCD-1mice[1]Dosage:1,5and50mg/kgAdministration:OraladministrationandintravenousinjectionResult:1.19parameter1mg/kgi.v.5mg/kgp.o.50mg/kgp.o.CL(mL/min/kg)27CLr户使⽤本产品发表的科研⽂献(mL/min/kg)5.3Vss•ActaPharmSinB.2020Dec15.(L/kg)2.3t1/2(h)tmax•EurJMedChem.2022Sep8;243:114683.(h)0.891.3Cmax•Aging.2020Nov3;12(21):21423-21445.(ng/mL)3454693AUC0-last(h·ng/mL)603128121158AUC0-Seemorecustomervalidationsonwww.MedChemEinf(h·ng/mL)616147921170REFERENCES[1].MitchellLH,et,al.NovelOxindoleSulfonamidesandSulfamides:EPZ03168Inhibitor.ACSMedChemLett.2015Aug27;7(2):134-8.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuse