H3B-8800-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEH3B-8800Cat.No.:HY-111517CASNo.:1825302-42-8分子式:C₃₁H₄₅N₃O₆分子量:555.71作用靶点:DNA/RNASynthesis;Apoptosis作用通路:CellCycle/DNADamage;Apoptosis储存方式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥100mg/mL(179.95mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM1.7995mL8.9975mL17.9950mL5mM0.3599mL1.7995mL3.5990mL10mM0.1799mL0.8997mL1.7995mL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。BIOLOGICALACTIVITY生物活性H3B-8800是一种有效的口服活性SF3B剪接(SF3Bsplicing)调节剂。H3B-8800与SF3b复合物直接相互作用并显示出抗癌活性。H3B-8800具有研究SF3B1突变体急性髓系白血病(AML)的潜力[1]。IC50&TargetSF3Bsplicing[1]1/2 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemE体外研究H3B-8800(0.1-10000nM;72h)inhibitscellgrowthinSF3B1-mutantcelllinePanc05.04cells[1].H3B-8800(0.1-10000nM;24h)inducesapoptosisinSF3B1-mutantcelllinePanc05.04cellsinadose-dependentmanner[1].ApoptosisAnalysis[1]CellLine:SF3B1-mutantcelllinePanc05.04cellsConcentration:0.1,1,10,100,1000,10000nMIncubationTime:24hResult:Inducedapoptosisbyincreasedcaspase-3/7cleavageinadose-dependentmanner.体内研究H3B-8800(2,4mg/kg;p.o.;daily)showsantitumoractivityinAMLderivedxenografts(PDXs)withamutationinSF3B1[1].AnimalModel:6-8weeks,femaleNSGorCB17-SCIDmice(K562cellswithSF3B1WTorSF3B1K700E)[1]Dosage:2,4mg/kgAdministration:P.o.;dailyResult:ResultedinantileukemicefficacyandsplicingmodulationinmicebearingAMLpatient-derivedxenografts(PDXs)withamutationinSF3B1buthadlittleeffectinmicebearingSF3B1WTAMLPDXs,significantlyreducedleukemicburdenrelativeinSF3B1K700EPDX.REFERENCESSeilerM,etal.H3B-8800,anorallyavailablesmall-moleculesplicingmodulator,induceslethalityinspliceosome-mutantcancers.NatMed.2018May;24(4):497-504.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel: