Lapatinib-GW572016-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemELapatinibCat.No.:HY-50898CASNo.:231277-92-2Synonyms:GW572016;GW2016分⼦式:C₂₉H₂₆ClFN₄O₄S分⼦量:581.06作⽤靶点:EGFR;Autophagy;Ferroptosis作⽤通路:JAK/STATSignaling;ProteinTyrosineKinase/RTK;Autophagy;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:125mg/mL(215.12mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.7210mL8.6050mL17.2099mL5mM0.3442mL1.7210mL3.4420mL10mM0.1721mL0.8605mL1.7210mL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)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(3.58mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.08mg/mL(3.58mM);Suspendedsolution;Needultrasonic3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.58mM);Clearsolution4.请依序添加每种溶剂：12%SBE-beta-CDSolubility:5mg/mL(8.60mM);Suspendedsolution;Needultrasonic5.请依序添加每种溶剂：5%DMSO>>95%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(4.30mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性Lapatinib(GW572016)⼀种ErbB-2和EGFR酪氨酸激酶结构域的有效抑制剂，对纯化的EGFR和ErbB-2的IC50值分别为10.2和9.8nM。IC50&TargetEGFRErbB210.2nM(IC50,CellFreeAssay)9.8nM(IC50,CellFreeAssay)体外研究Lapatinib(GW2016;0.03-10µM;6hours;BT474andHN5cells)treatmentinhibitsreceptorautophosphorylationofEGFRandErbB-2inadose-responsivemanner.Phosphorylationofserine473ofAKTwasinhibitedbyGW2016inadose-dependentmanner[1].Lapatinib(GW2016;72hours;HN5,A-43,BT474,N87,andCaLu-3cells)treatmenthasaselectiveinhibitionoftheproliferationofhumantumorcelllines[1].Lapatinib(GW2016;1-10µM;72hours;HN5cells)treatmentresultsininducesG1arrest[1].WesternBlotAnalysis[1]CellLine:BT474andHN5cellsConcentration:0.03µM,0.1µM,0.3µM,1µM,3µM,or10µMIncubationTime:6hoursResult:InhibitedreceptorautophosphorylationofEGFRandErbB-2inadose-responsivemanner.Phosphorylationofserine473ofAKTwasalsoinhibitedinadose-dependentmanner.CellProliferationAssay[1]CellLine:HN5,A-43,BT474,N87,andCaLu-3cellsConcentration:IncubationTime:72hours2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEResult:InhibitedthegrowthoftumorcellsoverexpressingEGFRorErbB-2.CellCycleAnalysis[1]CellLine:HN5cellsConcentration:1µM,or10µMIncubationTime:72hoursResult:ResultedininductionofG1arrest.体内研究Lapatinib(GW2016;30-100mg/kg;oraladministration;twicedaily;for21days;CD-1nudefemalemice)treatmentinhibitstumorxenograftgrowthoftheHN5cellsinadose-responsivemannerat30and100mg/kg,withcompleteinhibitionoftumorgrowthatthehigherdose[1].AnimalModel:CD-1nudefemalemice(4-6weeksold)withHN5cells[1]Dosage:30mg/kg,100mg/kgAdministration:Oraladministration;twicedaily;for21daysResult:InhibitedtumorxenograftgrowthoftheHN5cellsinadose-responsivemanner.户使⽤本产品发表的科研⽂献•NatMed.2016Jul;22(7):723-6.•Nature.2017Aug24;548(7668):471-475.•NatImmunol.2018Mar;19(3):233-245.•SciTranslMed.2018Jul18;10(450).pii:eaaq1093.•JExpClinCancerRes.2018Jun25;37(1):123.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].RusnakDW,etal.Theeffectsofthenovel,reversibleepidermalgrowthfactorreceptor/ErbB-2tyrosinekinaseinhibitor,GW2016,onthegrowthofhumannormalandtumor-derivedcelllinesinvitroandinvivo.MolCancerTher.2001Dec;1(2):85-94McePdfHeight