FGTI-2734-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEFGTI-2734Cat.No.:HY-128350CASNo.:1247018-19-4分?式:C??H??FN?O?S分?量:510.63作?靶點(diǎn):FarnesylTransferase作?通路:MetabolicEnzyme/Protease儲存?式:4°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:50mg/mL(97.92mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.9584mL9.7918mL19.5837mL5mM0.3917mL1.9584mL3.9167mL10mM0.1958mL0.9792mL1.9584mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month(storedundernitrogen)。-80°C儲存時(shí)，請?jiān)?個?內(nèi)使?，-20°C儲存時(shí)，請?jiān)?個?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥7.5mg/mL(14.69mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性FGTI-2734RASC-末端法尼轉(zhuǎn)移酶(FT)和?葉烯轉(zhuǎn)移酶-1(GGT-1)抑制劑，對FT和GGT-1的IC50s分別為250nM和520nM。FGTI-2734可以阻斷KRAS的膜定位，從?解決KRAS耐藥性問題，并抑制突變的KRAS胰腺腫瘤。IC50&TargetIC50:250nM(FT)and520nM(GGT-1)[1]體外研究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.體內(nèi)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?邊的抑制劑?師www.MedChemE[1].KaziA,etal.DualfarnesylandgeranylgeranyltransferaseinhibitorthwartsmutantKRAS-drivenpatient-derivedpancreatictumors.ClinCancerRes.2019Jun21.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplicat