UNC569-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEUNC569Cat.No.:HY-117596CASNo.:1350547-65-7分⼦式:C₂₂H₂₉FN₆分⼦量:396.5作⽤靶点:TAMReceptor作⽤通路:ProteinTyrosineKinase/RTK储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:31.25mg/mL(78.81mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.5221mL12.6103mL25.2207mL5mM0.5044mL2.5221mL5.0441mL10mM0.2522mL1.2610mL2.5221mL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>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.31mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性UNC569⼀种有效、可逆、ATP竞争性且具有⼝服活性的Mer激酶抑制剂，IC50为2.9nM，Ki为4.3nM。UNC569还抑制Axl和Tyro3，IC50分别为37nM和48nM。UNC569可⽤于急性淋巴细胞⽩⾎病(ALL)和⾮典型畸胎瘤/横纹肌瘤的研究。IC50&TargetIC50:2.9nM(Mer),37nM(Axl),48nM(Tyro3)[1]Ki:4.3nM(Mer)[1]体外研究UNC569(24hours)inducesapoptosisinALLcelllines,andincreasesthelevelsofcleavedCaspase3andcleavedPARP[2].UNC569(1µM;1.5hours)treatmenteffectivelyinhibittheactivationofMeranddownstreamsignaling,includingthePI3K/AKTandMAPK/ERKpathways[2].UNC569(1hour)inhibitsMerphosphorylationlevelswithIC50valuesof141nMand193nMinhumanB-ALL(acutelymphoblasticleukemia)697andJurkatcelllines,respectively[1][2].ApoptosisAnalysis[2]CellLine:697andJurkatcellsConcentration:0.4µM,0.8µM,1µM,1.2µM,1.4µM,1.6µM,1.8µM,2µMIncubationTime:24hoursResult:InducedapoptosisinALLcelllines.WesternBlotAnalysis[2]CellLine:697andJurkatcellsConcentration:1µMIncubationTime:1.5hoursResult:InhibitedMeractivationanddownstreamsignalingthroughERK1/2andAKT.体内研究TheinvivopharmacokineticpropertiesofUNC569(3mg/kg)arealsoassessedinmiceviabothintravenous(IV)andoral(PO)administration.UNC569haslowsystemicclearance(19.5mL/min/kg),highvolumeofdistribution(Vssof5.83L/kg),andgoodoralbioavailability(57%)[1].Leukemiczebrafisharetreatedcontinuouslyfor2weeksbyimmersionin4µMUNC569.theresultshowsthatUNC569inducesmorethan50%reductionintumorburdencomparedwithvehicle-andmock-treatedfish[2].REFERENCES[1].SandraChristoph,etal.UNC569,anovelsmall-moleculemerinhibitorwithefficacyagainstacutelymphoblasticleukemiainvitroandinvivo.MolCancerTher.2013Nov;12(11):2367-77.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[2].JingLiu,etal.DiscoveryofNovelSmallMoleculeMerKinaseInhibitorsfortheTreatmentofPediatricAcuteLymphoblasticLeukemia.ACSMedChemLett.2012Feb9;3(2):129-134.McePdfHeightCaution:Producthasnotbeenfullyvalidatedfor