Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemEAnticanceragent109Cat.No.:HY-149092CASNo.:2097497-16-8分子式:C??H??N?O?分子量:317.34作用靶點(diǎn):TAMReceptor;Others作用通路:ProteinTyrosineKinase/RTK;Others儲存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性Anticanceragent109(compound6-15)是Gas6-Axl軸的抑制劑，具有抑癌活性。Anticanceragent109抑制Gas6和Axl的表達(dá)，抑制p-PI3K和p-AKT的表達(dá)，導(dǎo)致腫瘤細(xì)胞周期G1期阻滯進(jìn)而促進(jìn)細(xì)胞凋亡(apoptosis)并在裸鼠荷瘤模型中顯著抑制腫瘤生長[1]。IC50&TargetAxl體外研究Anticanceragent109(10μM,48h)inhibitsofGas6andAxlinA549,inhibitsofGas6-Axlaxisrelatedproteins,increasesthesub-G1fractionandpromotesoflatestageapoptosiswithoutalteringDNAsynthesisinPANC-1[1].CellViabilityAssay[1]CellLine:MCF-7;PANC-1;MDA-MB-231;HT-29;DU145;U937;A549;PANC-1Concentration:30μMIncubationTime:48hResult:Inhibitedthegrowthofcancercells,andwasupto20-foldsaferagainstnormalcellsandupto5.4-foldmoreactivethanSunitinibagainstthecancercells.InhibitedgrowthwithIC50sof2.0μM(MCF-7);2.8μM(MDA-MB-231);4.6μM(HT-29);1.1μM(DU145);6.7μM(U937);4.2μM(A549);4.0μM(PANC-1).ApoptosisAnalysis[1]1/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemECellLine:PANC-1Concentration:1μM,5μM,10μMIncubationTime:48hResult:Increasedthesub-G1fractionandinducedlateapoptosis.WesternBlotAnalysis[1]CellLine:A549;PANC-1Concentration:10μMIncubationTime:48hResult:InhibitedGas6andAxlinA549andPANC-1cell,increasedtheexpressionratioofBax/Bcl-2andinhibitedp-PI3Kandp-AKTinPANC-1cell.RT-PCR[1]CellLine:PANC-1Concentration:3μM;5μM10μMIncubationTime:48hResult:InhibitedGas6andAxl.體內(nèi)研究Anticanceragent109(3mg/kg,intraperitonealinjection,A549tumormodelfor31days,PANC-1tumormodelfor85days,sixtimesaweek)reducedtumorsizeandweightsignificantlyinxenograftmodelsofnudemice[1].AnimalModel:A549orPANC-1xenograftedinBALB/c-numice[1].Dosage:1mg/kg;3mg/kgAdministration:Intraperitonealinjection(i.p.)6timesaweekResult:Promotedtumorregressiontoaroundaquarterwith1mg/kg,smallerbutnoteliminatedwith3mg/kginA549models.Promotedtumorregressiontoaroundaquarterwith3mg/kginPANC-1models.REFERENCES[1].BaeD,etal.Antitumoreffectof3-(quinolin-2-ylmethylene)-4,6-dimethyl-5-hydroxy-7-azaoxindoledown-regulatingtheGas6-Axlaxis.2/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEEurJMedChem.2023May5;251:115274.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications