FIDAS-5-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemEFIDAS-5Cat.No.:HY-136144CASNo.:1391934-98-7分⼦式:C₁₅H₁₃ClFN分⼦量:261.72作⽤靶点:Wnt作⽤通路:StemCell/Wnt储存⽅式:Powder-20°C3years4°C2years*该产品在溶液状态不稳定，建议您现⽤现配，即刻使⽤。溶解性数据体外实验DMSO:125mg/mL(477.61mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.8209mL19.1044mL38.2088mL5mM0.7642mL3.8209mL7.6418mL10mM0.3821mL1.9104mL3.8209mL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；该产品在溶液状态不稳定，建议您现⽤现配，即刻使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的⼯作液，建议您现⽤现配，当天使⽤；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分⽐指该溶剂在您配制终溶液中的体积占⽐)：1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(7.95mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(7.95mM);ClearsolutionBIOLOGICALACTIVITY1/2MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemE⽣物活性FIDAS-5⼀种有效的⼝服活性的甲硫氨酸腺苷转移酶2A(MAT2A)抑制剂，IC50为2.1μM。FIDAS-5与S-腺苷甲硫氨酸(SAM)有效竞争MAT2A结合，并具有抗癌活性。IC50&TargetIC50:2.1μM(MethionineS-adenosyltransferase2A(MAT2A))[1]体外研究FIDAS-5(3μM;7days;LS174Tcells)treatmentsignificantlyinhibitstheproliferationofLS174Tcells[1].FIDAS-5(3μM)treatmentinhibitstheexpressionofc-MycandcyclinD1inLS174TCRCcells.AndFIDAS-5inducestheexpressionofcellcycleinhibitor,p21WAF1/CIP1[1].FIDAS-5(3μM;36h)treatmentreducesthelevelsofbothS-adenosylmethionine(SAM)andS-adenosylhomocysteine(SAH)inLS174Tcells[1].CellViabilityAssay[1]CellLine:LS174Tcolorectalcancer(CRC)cellsConcentration:3μMIncubationTime:7daysResult:SignificantlyinhibitedtheproliferationofLS174Tcells.体内研究FIDAS-5(20mg/kg;oralgavage;daily;fortwoweeks;athymicnudemice)treatmentsignificantlyinhibitsthegrowthofxenografttumors,withminimaldifferenceinbodyweight[1].MicearetreatedwithFIDAS-5(20mg/kg)for1week.TheliverSAMlevelsaresignificantlyreduced[1].AnimalModel:16athymicnudemiceinjectedwithHT29CRCcells[1]Dosage:20mg/kgAdministration:Oralgavage;daily;fortwoweeksResult:Significantlyinhibitedthegrowthofxenografttumors.REFERENCES[1].ZhangW,etal.FluorinatedN,N-dialkylaminostilbenesrepresscoloncancerbytargetingmethionineS-adenosyltransferase2A.ACSChemBiol.2013Apr19;8(4):796-803.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forr