Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemETVB-3166Cat.No.:HY-120394CASNo.:1533438-83-3分?式:C??H??N?O分?量:384.47作?靶點:FattyAcidSynthase(FASN);Apoptosis作?通路:MetabolicEnzyme/Protease;Apoptosis儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:62.5mg/mL(162.56mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.6010mL13.0049mL26.0098mL5mM0.5202mL2.6010mL5.2020mL10mM0.2601mL1.3005mL2.6010mL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。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?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：(為保證實驗結果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；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>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(5.41mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.08mg/mL(5.41mM);Suspendedsolution;Needultrasonic3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.41mM);ClearsolutionBIOLOGICALACTIVITY?物活性TVB-3166?種?服有效，可逆和選擇性脂酸合成酶(FASN)抑制劑，對于FASN和細胞棕櫚酸酯合成的IC50分別為42nM和81nM。TVB-3166誘導細胞凋亡，并抑制體內(nèi)異種移植腫瘤的?長。IC50&TargetIC50:42nM(FASN)and81nM(cellularpalmitatesynthesis)[1]體外研究TVB-3166(0.001-10μM;24hours)causescelldeathinCALU-6non-small-celllungtumorcellswithacellularIC50valueof0.10μM[1].TVB-3166(0.02or0.20μM;7days)inhibitspalmitatesynthesisandtumorcellviabilityinadose-dependentmanner[1].TVB-3166(0.2μM;48hours)inhibitsβ-cateninpathwaysignaltransductionandtranscriptionalactivity[1].CellProliferationAssay[1]CellLine:CALU-6tumorcellsConcentration:0.001,0.01,0.1,1,10μMIncubationTime:24hoursResult:CausedcelldeathinCALU-6non-small-celllungtumorcellswithacellularIC50valueof0.10μM.CellViabilityAssay[1]CellLine:90differenttumorcelllines(suchasCALU-6NSCLCcellline,NCI-H1975NSCLCcellline)Concentration:0.02or0.20μMIncubationTime:7daysResult:Dose-dependentinductionofcelldeathwasobservedinalltumorcelllines.WesternBlotAnalysis[1]CellLine:COLO-205andA549cellsConcentration:0.2μMIncubationTime:48hours2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEResult:Inhibitedβ-cateninpathwaysignaltransductionandtranscriptionalactivity.體內(nèi)研究TVB-3166(Oralgavage;30-100mg/kg/day)inhibitsxenografttumorgrowth[1].TVB-3166(Oralgavage;30-100mg/kg/day)hastheconcentrationisapproximately3-foldhigherinplasmathantumor.The100and30mg/kggroupshadplasmaandtumorconcentrationsof7and2.9μM,respectively[1].AnimalModel:FemaleBALB-c-nudemice[1]Dosage:30,60,or100mg/kgAdministration:Oralgavage;oncedailyResult:Inhibitedxenografttumorgrowth.AnimalModel:FemaleBALB-c-nudemice[1]Dosage:30,60,or100mg/kg(PharmacokineticStudy)Administration:Oralgavage;oncedailyResult:Theconcentrationwasapproximately3-foldhigherinplasmathantumor.The100and30mg/kggroupshadplasmaandtumorconcentrationsof7and2.9μM,respectively.戶使?本產(chǎn)品發(fā)表的科研?獻?NatMetab.2021Sep27;1-10.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].VenturaR,etal.InhibitionofdenovoPalmitateSynthesisbyFattyAcidSynthaseInducesApoptosisinTumorCellsbyRemodelingCellMembranes,InhibitingSignalingPathways,andReprogrammingGeneExpression.EBioMedicine.2015Jul2;2(8):808-24.McePdfHeightCaution:Product