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Medchemexpress/Gefitinib(Synonyms: ZD1839)/HY-50895/1g

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Medchemexpress/Gefitinib(Synonyms: ZD1839)/HY-50895/1g

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MedChemExpress

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HY-50895-10mM*1mLinDMSO

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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

ConcentrationVolumeMass	1mg	5mg	10mg

1mM	2.2376mL	11.1882mL	22.3764mL
5mM	0.4475mL	2.2376mL	4.4753mL
10mM	0.2238mL	1.1188mL	2.2376mL

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°C	3years
	4°C	2years
Insolvent	-80°C	6months
	-20°C	1month

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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