MedKoo Biosciences/Canertinib/200600/50mg

Canertinibdihydrochlorideisthehydrochloridesaltofanorallybio-availablequinazolinewithpotentialantineoplasticandradiosensitizingactivities.Canertinibbindstotheintracellulardomainsofepidermalgrowthfactorreceptortyrosinekinases(ErbBfamily),irreversiblyinhibitingtheirsignaltransductionfunctionsandresultingintumorcellapoptosisandsuppressionoftumorcellproliferation.Thisagentalsoactsasaradiosensitizingagentanddisplayssynergisticactivitywithotherchemotherapeuticagents.

MedKooCat#:200600
Name:Canertinib
CAS#:289499-45-2(HClsalt)
ChemicalFormula:C24H27Cl3FN5O3
ExactMass:
MolecularWeight:558.86
ElementalAnalysis:C,51.58;H,4.87;Cl,19.03;F,3.40;N,12.53;O,8.59

Synonym:CI1033PD183805.

IUPAC/ChemicalName:N-(4-((3-Chloro-4-fluorophenyl)amino)-7-(3-(morpholin-4-yl)propoxy)quinazolin-6-yl)prop-2-enamide

InChiKey:OMZCMEYTWSXEPZ-UHFFFAOYSA-N

InChiCode:InChI=1S/C24H25ClFN5O3/c1-2-23(32)30-21-13-17-20(14-22(21)34-9-3-6-31-7-10-33-11-8-31)27-15-28-24(17)29-16-4-5-19(26)18(25)12-16/h2,4-5,12-15H,1,3,6-11H2,(H,30,32)(H,27,28,29)

SMILESCode:C=CC(NC1=CC2=C(NC3=CC=C(F)C(Cl)=C3)N=CN=C2C=C1OCCCN4CCOCC4)=O

TechnicalData

Appearance:

Solidpowder

Purity:

>98%(orrefertotheCertificateofAnalysis)

ShippingCondition:

Shippedunderambienttemperatureasnon-hazardouschemical.ThisproductisstableenoughforafewweeksduringordinaryshippingandtimespentinCustoms.

StorageCondition:

Dry,darkandat0-4Cforshortterm(daystoweeks)or-20Cforlongterm(monthstoyears).

Solubility:

SolubleinDMSO,notinwater

ShelfLife:

>5yearsifstoredproperly

DrugFormulation:

ThisdrugmaybeformulatedinDMSO

StockSolutionStorage:

0-4Cforshortterm(daystoweeks),or-20Cforlongterm(months).

HarmonizedSystemCode:

293490

AdditionalInformation

Related:
289499-45-2(CanertinibHClsallt)
267243-28-7(Canertinibfreebase).
Canertinib(CI-1033)isanexperimentaldrugcandidateforthetreatmentofcancer.Itisanirreversibletyrosine-kinaseinhibitorwithactivityagainstEGFR(IC500.8nM),HER-2(IC5019nM)andErbB-4(IC507nM).
Canertinib(CI-1033)isanexperimentaldrugcandidateforthetreatmentofcancer.Itisanirreversibletyrosine-kinaseinhibitorwithactivityagainstEGFR(IC500.8nM),HER-2(IC5019nM)andErbB-4(IC507nM).

References

1:MinochaM,KhuranaV,QinB,PalD,MitraAK.EnhancedbrainaccumulationofpazopanibbymodulatingP-gpandBcrp1mediatedeffluxwithcanertiniborerlotinib.IntJPharm.2012Oct15;436(1-2):127-34.doi:10.1016/j.ijpharm.2012.05.038.Epub2012Jun9.PubMedPMID:22688250.

2:DjerfSeverinssonEA,TrinksC,GrÃ©enH,AbdiuA,HallbeckAL,StÃ¥lO,WalzTM.Thepan-ErbBreceptortyrosinekinaseinhibitorcanertinibpromotesapoptosisofmalignantmelanomainvitroanddisplaysanti-tumoractivityinvivo.BiochemBiophysResCommun.2011Oct28;414(3):563-8.Epub2011Oct1.PubMedPMID:21982771.

3:NordigÃ¥rdenA,ZetterbladJ,TrinksC,GrÃ©enH,EliassonP,DruidP,LotfiK,RÃ¶nnstrandL,WalzTM,JÃ¶nssonJI.Irreversiblepan-ERBBinhibitorcanertinibelicitsanti-leukaemiceffectsandinducestheregressionofFLT3-ITDtransformedcellsinmice.BrJHaematol.2011Oct;155(2):198-208.doi:10.1111/j.1365-2141.2011.08819.x.Epub2011Aug16.PubMedPMID:21848891.

4:PrasasyaRD,VangKZ,KreegerPK.AmultivariatemodelofErbBnetworkcompositionpredictsovariancancercellresponsetocanertinib.BiotechnolBioeng.2012Jan;109(1):213-24.doi:10.1002/bit.23297.Epub2011Aug23.PubMedPMID:21830205.

5:TrinksC,SeverinssonEA,HolmlundB,GrÃ©enA,GrÃ©enH,JÃ¶nssonJI,HallbeckAL,WalzTM.Thepan-ErbBtyrosinekinaseinhibitorcanertinibinducescaspase-mediatedcelldeathinhumanT-cellleukemia(Jurkat)cells.BiochemBiophysResCommun.2011Jul8;410(3):422-7.Epub2011Jun6.PubMedPMID:21669187.

6:TrinksC,DjerfEA,HallbeckAL,JÃ¶nssonJI,WalzTM.Thepan-ErbBreceptortyrosinekinaseinhibitorcanertinibinducesErbB-independentapoptosisinhumanleukemia(HL-60andU-937)cells.BiochemBiophysResCommun.2010Feb26;393(1):6-10.Epub2010Jan22.PubMedPMID:20096663.

7:GalmariniCM.Canertinibpfizer.IDrugs.2004Jan;7(1):58-63.Review.PubMedPMID:14730468.

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MedKoo Biosciences/Canertinib/200600/50mg

TechnicalData

AdditionalInformation

References