B-I09-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEBI09Cat.No.:HY-107400CASNo.:1607803-67-7分⼦式:C₁₆H₁₇NO₅分⼦量:303.31作⽤靶点:IRE1作⽤通路:CellCycle/DNADamage储存⽅式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性数据体外实验DMSO:8.33mg/mL(27.46mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.2970mL16.4848mL32.9696mL5mM0.6594mL3.2970mL6.5939mL10mM0.3297mL1.6485mL3.2970mL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(protectfromlight)。-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>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(8.24mM);Suspendedsolution;Needultrasonic1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性BI09IRE-1核糖核酸酶的⼀个抑制剂，其IC50值为1230nM。IC50&TargetIC50:1230nM(IRE-1RNase)[1].体外研究BI09isanIRE-1RNaseinhibitor,withanIC50of1230nM[1].TreatmentofCLLcellswiththisinhibitor(BI09)mimickXBP-1deficiency,includingupregulationofIRE-1expressionandcompromisedBCRsignaling.BI09ishighlyeffectiveininhibitingsplicingofXBP1mRNAinhumanWaC3cellsandtheexpressionofXBP-1sinLPSstimulatedBcells[2].体内研究BI09hasahalflifeofapproximately1.5hoursandreachesitspeakconcentrationofapproximately39μMinmouseplasmaserum15minutesafteradministration.AdministrationofBI09toCLLtumor-bearingmicesuppressleukemicprogressionbyinducingapoptosisanddonotcausesystemictoxicity[2].PROTOCOLAnimalMice[2]Administration[2]MiceareintraperitoneallyinjectedwithBI09(50mg/kg)onthefirst5daysofeachweekfor3weeks[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•Patent.US20220381787A1.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].RanatungaS,etal.Synthesisofnoveltricyclicchromenone-basedinhibitorsofIRE-1RNaseactivity.JMedChem.2014May22;57(10):4289-301.[2].TangCH,etal.InhibitionofERstress-associatedIRE-1/XBP-1pathwayreducesleukemiccellsurvival.JClinInvest.2014Jun;124(6):2585-98.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forre