Lapatinib-GW572016-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemELapatinibCat.No.:HY-50898CASNo.:231277-92-2Synonyms:GW572016;GW2016分?式:C??H??ClFN?O?S分?量:581.06作?靶點:EGFR;Autophagy;Ferroptosis作?通路:JAK/STATSignaling;ProteinTyrosineKinase/RTK;Autophagy;Apoptosis儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:125mg/mL(215.12mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.7210mL8.6050mL17.2099mL5mM0.3442mL1.7210mL3.4420mL10mM0.1721mL0.8605mL1.7210mL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備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；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)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(3.58mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.08mg/mL(3.58mM);Suspendedsolution;Needultrasonic3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.58mM);Clearsolution4.請依序添加每種溶劑：12%SBE-beta-CDSolubility:5mg/mL(8.60mM);Suspendedsolution;Needultrasonic5.請依序添加每種溶劑：5%DMSO>>95%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(4.30mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性Lapatinib(GW572016)?種ErbB-2和EGFR酪氨酸激酶結(jié)構(gòu)域的有效抑制劑，對純化的EGFR和ErbB-2的IC50值分別為10.2和9.8nM。IC50&TargetEGFRErbB210.2nM(IC50,CellFreeAssay)9.8nM(IC50,CellFreeAssay)體外研究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?邊的抑制劑?師www.MedChemEResult:InhibitedthegrowthoftumorcellsoverexpressingEGFRorErbB-2.CellCycleAnalysis[1]CellLine:HN5cellsConcentration:1μM,or10μMIncubationTime:72hoursResult:ResultedininductionofG1arrest.體內(nèi)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.戶使?本產(chǎn)品發(fā)表的科研?獻?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