Tetrac-Tetraiodothyroacetic-acid-DataSheet-生命科学试剂-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemETetracCat.No.:HY-W008859CASNo.:67-30-1Synonyms:Tetraiodothyroaceticacid;3,3',5,5'-Tetraiodothyroaceticacid分⼦式:C₁₄H₈I₄O₄分⼦量:747.83作⽤靶点:EndogenousMetabolite作⽤通路:MetabolicEnzyme/Protease储存⽅式:-20°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性数据体外实验DMSO:100mg/mL(133.72mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.3372mL6.6860mL13.3720mL5mM0.2674mL1.3372mL2.6744mL10mM0.1337mL0.6686mL1.3372mL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，并请注意储备液的保存⽅式和期限。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，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的⼯作液，建议您现⽤现配，当天使⽤；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分⽐指该溶剂在您配制终溶液中的体积占⽐)：1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:2.5mg/mL(3.34mM);Suspendedsolution;Needultrasonic2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(3.34mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(3.34mM);Clearsolution1/3MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性Tetrac(Tetraiodothyroaceticacid)，L-甲状腺素(T4)的脱氨类似物，甲状腺素整合素受体拮抗剂。Tetrac阻断T3和T4的作⽤以及不同的⽣长因⼦介导的⾎管⽣成。Tetra还具有抗肿瘤活性。体外研究Tetrac(0.01-1μM;2-6d)inducesanti-proliferationinHT-29andHCT116cellswithdifferentK-RASstatus[3].Tetrac(0.1μM;30min)inhibitsactivationofERK1/2inHT-29andHCT116cells[3].Tetrac(0.1μM;24h)inhibitsexpressionofCCND1andc-Myc,butpromotesexpressionofCASP2andTHBS1[3].CellProliferationAssay[3]CellLine:HT-29andHCT116cellsConcentration:0.01,0.1,1μMIncubationTime:0,2,4,6daysResult:Inducedanti-proliferationofK-RASwild-typecolorectalcancercells.WesternBlotAnalysis[3]CellLine:HT-29andHCT116cellsConcentration:0.1μMIncubationTime:30minResult:InhibitedconstitutivelyactivatedERK1/2,andthisinhibitioncanremovebyanti-integrinαvβ3antibodypretreatment.体内研究Tetrac(35μg;p.o.for40days)inhibitstumorinoculation,growthandintegrinexpressioninmice[4].AnimalModel:Wild-typemaleBalb/Cmiceaged8weeksareinoculatedwith102B16F10orB16LS9cells[4]Dosage:35μgperdayAdministration:P.o.(addedtothedrinkingwater)dailyfor40daysResult:Delayedtheonsetofocularmelanoma.ReducedtheS-100andintegrinstaininglevelintheB16F10micemodel.REFERENCES2/3MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].SchmohlKA,et,al.Tetracasananti-angiogenicagentincancer.EndocrRelatCancer.2019Jun1;26(6):R287-R304.[2].DavisPJ,et,al.NongenomicActionsofThyroidHormone:theIntegrinComponent.PhysiolRev.2020Jun25.[3].ChinYT,et,al.TetracandNDATInduceAnti-proliferationviaIntegrinαvβ3inColorectalCancersWithDifferentK-RASStatus.FrontEndocrinol(Lausanne).2019Mar12;10:130.[4].Ashur-FabianO,et,al.TetracDelayedtheOnsetofOcularMelanomainanOrthotopicMouseModel.FrontEndocrinol(Lausanne).2019Jan8;9:775.[5].RajabiM,et,al.Synthesisofnewanalogsoftetraiodothyroaceticacid(tetrac)asnovelangiogenesisinhibitorsfortreatmentofcancer.BioorgMedChemLett.2018Apr15;28(7):1223-1227.McePdfHeightCaution:Producthasnotbeenful