MedKoo Biosciences/E7820/201090/2g

Synonym:E7820;E-7820;E7820.

IUPAC/ChemicalName:N-(3-cyano-4-methyl-1H-indol-7-yl)-3-cyanobenzene-sulfonamide

InChiKey:LWGUASZLXHYWIV-UHFFFAOYSA-N

InChiCode:InChI=1S/C17H12N4O2S/c1-11-5-6-15(17-16(11)13(9-19)10-20-17)21-24(22,23)14-4-2-3-12(7-14)8-18/h2-7,10,20-21H,1H3

SMILESCode:O=S(C1=CC=CC(C#N)=C1)(NC2=CC=C(C)C3=C2NC=C3C#N)=O

TechnicalData

AdditionalInformation

OraladmiNISTrationofE7820significantlyinhibitedbasicfibroblastgrowthfactor-inducedangiogenesisinMatrigelimplantsandhumancolonWiDrtumor-inducedangiogenesisinadorsalairsacmodel.Twice-dailytreatmentwithE7820clearlyinhibitedthes.c.tumorgrowthofseventumorcelllinesderivedfromhumancolon,breast,pancreas,andkidney,andcompletelysuppressedthegrowthofhumanpancreaticKP-1andhumancolonLoVocelllines.Moreover,E7820significantlyinhibitedthegrowthofKP-1andhumancolontumorColo320DMcellsorthotopicallyimplantedinthepancreasandcecum,respectively.TheefficacyofE7820wascomparableinthes.c.andorthotopictransplantationmodels.Immunohistochemicalanalysesusinganti-CD31antibodyshowedthatE7820significantlyreducedmicrovesseldensityinorthotopicallyimplantedKP-1tumor.E7820reducedintegrinalpha2expressiononamegakaryocyticcellline,Damicells,inducedbyphorbol12-myristate13-acetatetreatment.Italsodecreasedtheexpressionlevelofintegrinalpha2onplateletswithdrawnfrommicebearings.c.KP-1tumoratadosageclosetothataffordingantitumoractivity.ThesedatademonstratethatE7820showedabroad-spectrumantitumoreffectinmicethroughinhibitionofangiogenesisandindicatethatthedecreaseofintegrinalpha2onplateletsmightserveasaBIOLOGicalMarkerfortheantitumorefficacyofE7820.seehttp://www.ncbi.nlm.nih.gov/pubmed/14977846
    

References

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