SGX-523-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemESGX-523Cat.No.:HY-12019CASNo.:1022150-57-7分⼦式:C₁₈H₁₃N₇S分⼦量:359.41作⽤靶点:c-Met/HGFR作⽤通路:ProteinTyrosineKinase/RTK储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:30mg/mL(83.47mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.7823mL13.9117mL27.8234mL5mM0.5565mL2.7823mL5.5647mL10mM0.2782mL1.3912mL2.7823mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验SGX-523ispreparedin0.5%sodiumcarboxymethylcellulose[2].BIOLOGICALACTIVITY⽣物活性SGX523⼀种选择性和ATP竞争性的MET抑制剂。SGX523有效抑制MET，IC50为4nM，⽐作⽤于其它他蛋⽩激酶的选择性⾼于1,000倍。具有抗肿瘤特性[1]。1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE体外研究SGX523showsATP-competitiveinhibitionwithhigherapparentaffinityforthelessactive,unphosphorylatedformofMET[MET-KD(0P),Ki=2.7nM]versusthemoreactivephospho-enzyme[MET-KD(3P),Ki=23nM][1].SGX523inhibitsthegrowthofgastricandlungcancercelllineswithamplificationoftheMETgenebuthasnoeffect,evenathighmicromolarconcentration,oncelllineswithnormalMETgenecopynumber.TheIC50sof0.02,0.113,and0.035µMforNSCLCH1993,gastriccncerMKN45,andgastriccancerHs746Tcells,respectively[1].TheIC50valuefortheinhibitionofMETautophosphorylationis0.040μMinGTL16cells[1].SGX523(0.5,1.5,4.6,13.7,41,123,370,1100,3300,10000nM;1hour)inhibitsMETautophosphorylationwithoutaffectingtotalMETorextracellularsignal-regulatedkinaseproteinlevelsinHGF-stimulatedA549cells[1].CellViabilityAssay[1]CellLine:GastriccancercelllineGTL16Concentration:4.6,14,40,120,370,1100,3300,10000nMIncubationTime:1hoursResult:AbolishedconstitutivesignalinginducedbyMETgeneamplification.体内研究SGX523exhibitsantitumoractivityinvivo.SGX523inhibitsMET-dependenttumorgrowth[2].AnimalModel:FemaleHarlannudemice(athymicnu/nu)weres.c.implantedwithU87cells[2]Dosage:10or30mg/kgAdministration:Oralgavage;twicedailystartingatday5for22daysResult:PotentlyinhibitedU87MGtumorgrowthatadoseof10mg/kgadministeredtwicedaily.LedtoclearregressionofU87MGtumorsat30mg/kgdosedtwicedaily.户使⽤本产品发表的科研⽂献•Science.2017Dec1;358(6367):eaan4368.•SciTranslMed.2018Jul18;10(450).pii:eaaq1093.•CancerRes.2015Nov1;75(21):4548-59.•HarvardMedicalSchoolLINCSLIBRARYSeemorecustomervalidationsonwww.MedChemEREFERENCES[1].BuchananSG,etal.SGX523isanexquisitelyselective,ATP-competitiveinhibitoroftheMETreceptortyrosinekinasewithantitumor2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEactivityinvivo.MolCancerTher,2009,8(12),3181-3190.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedi