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Medchemexpress/Gefitinib(Synonyms: ZD1839)/HY-50895/500mg

GefitinibisaninhibitorthatspecificallybindsandinhibitstheEGFRtyrosinekinase,withtheIC50valueof2-37nMinNR6wtEGFRcells.

CustomerValidation

  • •StemCellReports.2017Nov23.pii:S2213-6711(17)30483-6.
  • •BreastCancerRes.2017Aug4;19(1):90.
  • •Oncotarget.2016Oct25;7(43):69760-69769.
  • •Oncotarget.2015Oct13;6(31):31313-22.
  • •ExpCellRes.2017Oct26.pii:S0014-4827(17)30574-8.
  • •JSepSci.2017Oct;40(19):3782-3791.
  • •BiomedChromatogr.2016Jul;30(7):1150-4.
  • •ChemPharmBull(Tokyo).2017Aug1;65(8):768-775.
  • •HarvardMedicalSchoolLINCSLIBRARY
Description

GefitinibisaninhibitorthatspecificallybindsandinhibitstheEGFRtyrosinekinase,withtheIC50valueof2-37nMinNR6wtEGFRcells.

IC50&Target

IC50:37nM (Tyr1173site,inNR6wtEGFRcells),37nM (Tyr992site,inNR6wtEGFRcells)[1]

InVitro

Gefitinib(0.01-0.1mM)resultsinincreasedphosphotyrosineloadofthereceptor,increasedsignallingtoERKandstimulationofproliferationandanchorage-independentgrowth,presumablybyinducingEGFRvIIIdimerisationinlong-termexposureofEGFRvIII-expressingcells.Ontheotherhand,gefitinib(1-2mM)significantlydecreasesEGFRvIIIphosphotyrosineload,EGFRvIII-mediatedproliferationandanchorage-independentgrowth[1].Gefitinib(ZD1839)inhibitsthemonolayergrowthoftheseEGF-drivenuntransformedcellswithIC50of20nM[2].GefitinibleadstoaninhibitionofCALU-3andGLC82cellproliferation,withanIC50of2μM[3].

InVivo

Gefitinib(150mg/kg,p.o.)inconbinationwithMetformininducesasignificantreductionintumorgrowthinnudemicebearingH1299orCALU-3GEF-Rcellsthataregrownsubcutaneouslyastumorxenografts[3].InirrADIatedrats,Gefitinibtreatmentaugmenteslunginflammation,includinginflammatorycellinfiltrationandpro-inflammatorycytokineexpression,whileGefitinibtreatmentattenuatesfibroticlungremodelingduetotheinhibitionoflungfibroblastproliferation[4].

ClinicalTrial
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References

  • [1].PedersenMW,etal.DifferentialresponsetogefitinibofcellsexpressingnormalEGFRandthemutantEGFRvIII.BrJCancer.2005Oct17;93(8):915-23.

    [2].MoasserMM,etal.ThetyrosinekinaseinhibitorZD1839("Iressa")inhibitsHER2-drivensignalingandsuppressesthegrowthofHER2-overexpressingtumorcells.CancerRes.2001Oct1;61(19):7184-8.

    [3].MorgilloF,etal.Synergisticeffectsofmetformintreatmentincombinationwithgefitinib,aselectiveEGFRtyrosinekinaseinhibitor,inLKB1wild-typeNSCLCcelllines.ClinCancerRes.2013Jul1;19(13):3508-19.

    [4].MiyakeK,etal.Epidermalgrowthfactorreceptor-tyrosinekinaseinhibitor(gefitinib)augmentspneumonitis,butattenuateslungfibrosisinresponsetoradiationinjuryinrats.JMedInvest.2012;59(1-2):174-85.

    [5].NohCK,etal.SimultaneousquantificationofvolitinibandgefitinibinratplasmabyHPLC-MS/MSforapplicationtoapharmacokineticstudyinrats.JSepSci.2017Jul27.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM2.2376mL11.1882mL22.3764mL
5mM0.4475mL2.2376mL4.4753mL
10mM0.2238mL1.1188mL2.2376mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
CellAssay
[3]

GefitinibisdissolvedinDMSOandstored,andthendilutedwithappropriatemediabeforeuse[3].

Cancercellsareseededin96-wellplatesandaretreatedwithdifferentdosesofGefitinib(0.01-20μM),Metforminorbothfor72hours.CellproliferationismeasuredwiththeMTTassay.TheIC50valuesaredeterminedbyinterpolationfromthedose-responsecurves.Resultsrepresentthemedianof3separateexperimentseachconductedinquadruplicate.TheresultsofthecombinedtreatmentareanalyzedaccordingtothemethodofChouandTalalaybyusingtheCalcuSynsoftwareprogram[3].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdmiNISTration
[3][4]

GefitinibissUSPendedin0.1%Tween80solution[4].

Mice[3]
Four-to6-weekoldfemalebalb/cathymic(nu+/nu+)miceareacclimatizedfor1weekbeforebeinginjectedwithcancercellsandinjectedsubcutaneouslywith107H1299andCALU-3GEF-Rcellsthathasbeenresuspendedin200μLofMatrigel.Whenestablishedtumorsofapproximately75mm3indiameteraredetected,miceareleftuntreatedortreatedwithoraladministrationsofmetformin(200mg/mLmetformindilutedindrinkingwaterandpresentthroughouttheexperiment),gefitinib(150mg/kgdailyorallybygavage),orbothfortheindicatedtimeperiods.Eachtreatmentgroupconsistsof10mice.Tumorvolumeismeasuredusingtheformulaπ/6×largerdiameter×(smallerdiameter)2.
Rat[4]
Theratsarerandomlyassignedto1of4experimentalgroups:1)theunirradiatedratstreatedwithoraladministrationofvehicle(0.1%Tween80)oncedaily;2)theunirradiatedratstreatedwithoraladministrationofgefitinib(50mg/kg/day)oncedaily;3)theirradiatedratstreatedwithoraladministrationofvehicleoncedaily;4)theirradiatedratstreatedwithoraladministrationofgefitiniboncedaily.Eachexperimentalgroupcomprised5-6ratsandalltreatmentsaredeliveredfor14days.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].PedersenMW,etal.DifferentialresponsetogefitinibofcellsexpressingnormalEGFRandthemutantEGFRvIII.BrJCancer.2005Oct17;93(8):915-23.

    [2].MoasserMM,etal.ThetyrosinekinaseinhibitorZD1839("Iressa")inhibitsHER2-drivensignalingandsuppressesthegrowthofHER2-overexpressingtumorcells.CancerRes.2001Oct1;61(19):7184-8.

    [3].MorgilloF,etal.Synergisticeffectsofmetformintreatmentincombinationwithgefitinib,aselectiveEGFRtyrosinekinaseinhibitor,inLKB1wild-typeNSCLCcelllines.ClinCancerRes.2013Jul1;19(13):3508-19.

    [4].MiyakeK,etal.Epidermalgrowthfactorreceptor-tyrosinekinaseinhibitor(gefitinib)augmentspneumonitis,butattenuateslungfibrosisinresponsetoradiationinjuryinrats.JMedInvest.2012;59(1-2):174-85.

    [5].NohCK,etal.SimultaneousquantificationofvolitinibandgefitinibinratplasmabyHPLC-MS/MSforapplicationtoapharmacokineticstudyinrats.JSepSci.2017Jul27.

MolecularWeight

446.9

Formula

C₂₂H₂₄ClFN₄O₃

CASNo.

184475-35-2

Storage
Powder-20°C3years
 4°C2years
Insolvent-80°C6months
 -20°C1month
Shipping

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

DMSO:≥30mg/mL

GefitinibisdissolvedinadosingvehiclecomposedofDMSO,PEG400,anddistilledwater(5:45:50%,v/v/v)attheconcentrationof1mg/mL[5].

*"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">

References

  • [1].PedersenMW,etal.DifferentialresponsetogefitinibofcellsexpressingnormalEGFRandthemutantEGFRvIII.BrJCancer.2005Oct17;93(8):915-23.

    [2].MoasserMM,etal.ThetyrosinekinaseinhibitorZD1839("Iressa")inhibitsHER2-drivensignalingandsuppressesthegrowthofHER2-overexpressingtumorcells.CancerRes.2001Oct1;61(19):7184-8.

    [3].MorgilloF,etal.Synergisticeffectsofmetformintreatmentincombinationwithgefitinib,aselectiveEGFRtyrosinekinaseinhibitor,inLKB1wild-typeNSCLCcelllines.ClinCancerRes.2013Jul1;19(13):3508-19.

    [4].MiyakeK,etal.Epidermalgrowthfactorreceptor-tyrosinekinaseinhibitor(gefitinib)augmentspneumonitis,butattenuateslungfibrosisinresponsetoradiationinjuryinrats.JMedInvest.2012;59(1-2):174-85.

    [5].NohCK,etal.SimultaneousquantificationofvolitinibandgefitinibinratplasmabyHPLC-MS/MSforapplicationtoapharmacokineticstudyinrats.JSepSci.2017Jul27.

Purity:99.95%

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