FGTI-2734-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEFGTI-2734Cat.No.:HY-128350CASNo.:1247018-19-4分⼦式:C₂₆H₃₁FN₆O₂S分⼦量:510.63作⽤靶点:FarnesylTransferase作⽤通路:MetabolicEnzyme/Protease储存⽅式:4°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性数据体外实验DMSO:50mg/mL(97.92mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.9584mL9.7918mL19.5837mL5mM0.3917mL1.9584mL3.9167mL10mM0.1958mL0.9792mL1.9584mL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(storedundernitrogen)。-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>>90%cornoilSolubility:≥7.5mg/mL(14.69mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性FGTI-2734RASC-末端法尼转移酶(FT)和⾹叶烯转移酶-1(GGT-1)抑制剂，对FT和GGT-1的IC50s分别为250nM和520nM。FGTI-2734可以阻断KRAS的膜定位，从⽽解决KRAS耐药性问题，并抑制突变的KRAS胰腺肿瘤。IC50&TargetIC50:250nM(FT)and520nM(GGT-1)[1]体外研究FGTI-2734(1-30μM;72hours)inducesCASPASE-3andPARPcleavageinMiaPaCa2,L3.6plandCalu6cells[1].FGTI-2734(3-30μM;72hours)inhibitsbothproteinprenylationofHDJ2,RAP1A,KRASandNRAS.FGTI-2734inhibitsKRASmembranelocalizationinRAS-transformedmurineNIH3T3cellsandinmutantKRAShumancancercells[1].ApoptosisAnalysis[1]CellLine:MiaPaCa2,L3.6plandCalu6cellsConcentration:1,3,10,30μMIncubationTime:72hoursResult:InducedCASPASE-3andPARPcleavageinMiaPaCa2,L3.6plandCalu6cells.WesternBlotAnalysis[1]CellLine:KRAS,HRAS,andNRAS-transformedNIH3T3cellsConcentration:3,10,30μMIncubationTime:72hoursResult:InhibitedbothproteinprenylationofHDJ2,RAP1A,KRASandNRAS.体内研究FGTI-2734(intraperitoneally;100mg/kg/dailyfor18to25days)onlyinhibitstumorgrowthinmutantKRAS-dependenttumorsbutnotinmutantKRAS-independenttumors[1].AnimalModel:MaleSCID-bgmicefollowinginjectionofMiaPaCa2,L3.6pl,Calu6,A549,H460andDLD1cancercells[1]Dosage:100mg/kgAdministration:Intraperitoneally;daily;for18to25daysResult:InhibitedtumorgrowthinmutantKRAS-dependenttumors.REFERENCES2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].KaziA,etal.DualfarnesylandgeranylgeranyltransferaseinhibitorthwartsmutantKRAS-drivenpatient-derivedpancreatictumors.ClinCancerRes.2019Jun21.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplicat