Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEVactosertibCat.No.:HY-19928CASNo.:1352608-82-2Synonyms:EW-7197;TEW-7197分?式:C??H??FN?分?量:399.42作?靶點:TGF-βReceptor作?通路:TGF-beta/Smad儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:100mg/mL(250.36mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.5036mL12.5182mL25.0363mL5mM0.5007mL2.5036mL5.0073mL10mM0.2504mL1.2518mL2.5036mL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。-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(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：(為保證實驗結(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)實驗的?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>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:2.5mg/mL(6.26mM);Suspendedsolution;Needultrasonic2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.26mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.26mM);ClearsolutionBIOLOGICALACTIVITY?物活性Vactosertib(EW-7197)?種有效的，具有?服活性且具有ATP競爭性激活素受體樣激酶5(ALK5)抑制劑，IC50為12.9nM。Vactosertib還以納爾濃度抑制ALK2和ALK4(IC50為17.3nM)。Vactosertib具有強?的抗轉(zhuǎn)移活性和抗癌作?。IC50&TargetALK512.9nM(IC50)體外研究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.體內(nèi)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?邊的抑制劑?師www.MedChemEAnimalModel:Mammarytumorvirus(MMTV)/c-Neufemalemice(32-week-old)[1]Dosage:40mg/kgAdministration:Intraperitonealinjection;everyotherday;for10weeksResult:InhibitedSmad/TGFβsignaling,cellmigration,invasion,andlungmetastasisinMMTV/c-Neumice.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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