B-I09-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEBI09Cat.No.:HY-107400CASNo.:1607803-67-7分?式:C??H??NO?分?量:303.31作?靶點(diǎn):IRE1作?通路:CellCycle/DNADamage儲(chǔ)存?式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:8.33mg/mL(27.46mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM3.2970mL16.4848mL32.9696mL5mM0.6594mL3.2970mL6.5939mL10mM0.3297mL1.6485mL3.2970mL請根據(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(protectfromlight)。-80°C儲(chǔ)存時(shí)，請?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(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.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(8.24mM);Suspendedsolution;Needultrasonic1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性BI09IRE-1核糖核酸酶的?個(gè)抑制劑，其IC50值為1230nM。IC50&TargetIC50:1230nM(IRE-1RNase)[1].體外研究BI09isanIRE-1RNaseinhibitor,withanIC50of1230nM[1].TreatmentofCLLcellswiththisinhibitor(BI09)mimickXBP-1deficiency,includingupregulationofIRE-1expressionandcompromisedBCRsignaling.BI09ishighlyeffectiveininhibitingsplicingofXBP1mRNAinhumanWaC3cellsandtheexpressionofXBP-1sinLPSstimulatedBcells[2].體內(nèi)研究BI09hasahalflifeofapproximately1.5hoursandreachesitspeakconcentrationofapproximately39μMinmouseplasmaserum15minutesafteradministration.AdministrationofBI09toCLLtumor-bearingmicesuppressleukemicprogressionbyinducingapoptosisanddonotcausesystemictoxicity[2].PROTOCOLAnimalMice[2]Administration[2]MiceareintraperitoneallyinjectedwithBI09(50mg/kg)onthefirst5daysofeachweekfor3weeks[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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