FT113-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEFT113Cat.No.:HY-111551CASNo.:1630808-89-7分⼦式:C₂₂H₂₀FN₃O₄分⼦量:409.41作⽤靶点:FattyAcidSynthase(FASN)作⽤通路:MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:62.5mg/mL(152.66mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.4425mL12.2127mL24.4254mL5mM0.4885mL2.4425mL4.8851mL10mM0.2443mL1.2213mL2.4425mL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。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(5.08mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.08mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性FT113⼀种有效、可⼝服的脂酸合酶(fattyacidsynthase(FASN))抑制剂，对全长重组⼈FASN酶的IC50值为213nM。在BT474细胞中，FT113抑制FASN的活性，IC50值为90nM。FT113具有抗增殖作⽤，在体内和体外实验中，都具有抗癌作⽤[1]。IC50&TargetIC50:213nM(FASN),90nM(FASN,inBT474cell)[1]体外研究FT113showsanti-proliferativeactivityagainstPC3andMV-411cellswithIC50sof47and26nM,respectively[1].体内研究FT113(5mg/kg,p.o.)exhibitspotentoralbioavailabilityof95%and84%inmiceandrats,respectively[1].FT113(5,25,or50mg/kg,p.o.,twicedailyfor16days)increasesmalonyl-CoAconcentrationintumors,inhibitstumorgrowthinadose-dependentmannerinmice[1].AnimalModel:AthymicnudemicebearingMV-411cells[1]Dosage:5,25,or50mg/kgAdministration:P.O.,twicedailyfor16daysResult:Caused32%and50%tumorgrowthinhibitionat25and50mg/kg,respectivelyinmice.REFERENCES[1].MartinMW,etal.Discoveryandoptimizationofnovelpiperazinesaspotentinhibitorsoffattyacidsynthase(FASN).BioorgMedChemLett.2019Apr15;29(8):1001-1006.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly