Vactosertib-EW-7197-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEVactosertibCat.No.:HY-19928CASNo.:1352608-82-2Synonyms:EW-7197;TEW-7197分⼦式:C₂₂H₁₈FN₇分⼦量:399.42作⽤靶点:TGF-βReceptor作⽤通路:TGF-beta/Smad储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(250.36mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.5036mL12.5182mL25.0363mL5mM0.5007mL2.5036mL5.0073mL10mM0.2504mL1.2518mL2.5036mL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%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:2.5mg/mL(6.26mM);Suspendedsolution;Needultrasonic2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.26mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.26mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Vactosertib(EW-7197)⼀种有效的，具有⼝服活性且具有ATP竞争性激活素受体样激酶5(ALK5)抑制剂，IC50为12.9nM。Vactosertib还以纳尔浓度抑制ALK2和ALK4(IC50为17.3nM)。Vactosertib具有强⼤的抗转移活性和抗癌作⽤。IC50&TargetALK512.9nM(IC50)体外研究Vactosertib(10-1000nM;30minutes;4T1cells)treatmentblockstheTGFβ-inducedphosphorylationofSmad2orSmad3inadose-dependentmannerin4T1cells[1].VactosertibsuppressestheTGFβ-inducednucleartranslocationofSmad2/3in4T1cellsandMCF10Acells.TheIC50valueofVactosertibonpSmad3in4T1cellsis10-30nM[1].VactosertibabrogatesTGFb1-inducedtumorcellmigrationandinvasion[1].TGFβ1downregulatedthemRNAlevelofCDH1andupregulatedthemRNAlevelsofFN1,HMGA2(high-mobilitygroupAT-hook2),SNAI1,andSNAI2(Snailfamilyzincfinger1and2,respectively).Moreover,VactosertibabolishestheTGFβ1-inducedeffectsongenesrelatedtoepithelial-to-mesenchymaltransition(EMT)[1].WesternBlotAnalysis[1]CellLine:4T1cellsConcentration:10nM,30µM,50nM,100µM,300nM,500nM,1000nMIncubationTime:30minutesResult:BlockedtheTGFb-inducedphosphorylationofSmad2orSmad3inadose-dependentmanner.体内研究Vactosertib(40mg/kg;intraperitonealinjection;everyotherday;for10weeks;MMTV/c-Neufemalemice)treatmentinhibitsSmad/TGFβsignaling,cellmigration,invasion,andlungmetastasisinMMTV/c-Neumice[1].Vactosertibalsoinhibitstheepithelial-to-mesenchymaltransition(EMT)inbothTGFβ-treatedbreastcancercellsand4T1orthotopic-graftedmice.Furthermore,VactosertibenhancescytotoxicTlymphocyteactivityin4T1orthotopic-graftedmiceandincreasedthesurvivaltimeof4T1-Lucand4T1breasttumor-bearingmice[1].2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAnimalModel:Mammarytumorvirus(MMTV)/c-Neufemalemice(32-week-old)[1]Dosage:40mg/kgAdministration:Intraperitonealinjection;everyotherday;for10weeksResult:InhibitedSmad/TGFβsignaling,cellmigration,invasion,andlungmetastasisinMMTV/c-Neumice.户使⽤本产品发表的科研⽂献•CellDiscov.2022Sep20;8(1):94.•Cancers.2020Jun30;12(7):1737.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].SonJYetal.EW-7197,anovelALK-5kinaseinhibitor,potentlyinhibitsbreasttolungmetastasis,2014Jul,13(7):1704-16.[2].NakaK,etal.Noveloraltransforminggrowthfactor-βsignalinginhibitorEW-7197eradicatesCML-initiatingcells.CancerSci.2016Feb;107(2):140-8.McePdfHeightCaution:Produc