TTT-28-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemETTT-28Cat.No.:HY-101511CASNo.:1609138-51-3分?式:C??H??N?O?S分?量:573.66作?靶點:P-glycoprotein作?通路:MembraneTransporter/IonChannel儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:250mg/mL(435.80mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.7432mL8.7160mL17.4319mL5mM0.3486mL1.7432mL3.4864mL10mM0.1743mL0.8716mL1.7432mL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?。BIOLOGICALACTIVITY?物活性TTT-28?種噻唑-纈氨酸肽模擬物，?效ABCB1(P-gp/MDR1)選擇性抑制劑，低毒性。TTT-28通過選擇性阻斷ATP結(jié)合盒亞家族B成員1(ABCB1)的外排功能,逆轉(zhuǎn)ABCB1介導(dǎo)的多藥耐藥性(MDR)。體外研究TTT-28(0-100?μM;72hours)reversesABCB1-mediatedMDRindrugselectedSW620/Ad300cellsandtransfectedHEK293/ABCB1cells;theIC50sofTTT-28inCCD-18Co,SW620andSW620/Ad300cellsare1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE213.4±11.0μM,89.4±3.9μMand92.0±5.0?μM,respectively[1].TTT-28(10μM;2hours)raisestheABCB1-mediatedMDRandincreasedtheaccumulationof[3H]-paclitaxelinABCB1overexpressingcells[1].TTT-28(10μM;0-72hours)doesnotinterferwiththeexpressionlevelandlocalizationofABCB1,itresultsfromblockingtheeffluxfunctionofABCB1[1].TTT-28(0-40?μM;2hours)interactsatthedrug-substrate-bindingsiteandactivestheATPaseactivityofABCB1inaconcentration-dependentfashion[1].CellViabilityAssay[1]CellLine:SW620cells,SW620/Ad300cellsConcentration:0.1?μM,1?μM,10?μM,100?μMIncubationTime:72hoursResult:DecreasedtheresistancefoldofABCB1substrates(Paclitaxel,Doxorubicin,Vincristine)inSW620/Ad300cellscomparedtoSW620cells.體內(nèi)研究TTT-28(deliverorally;30mg/kg;every3rdday;18days)potentiatestheanticanceractivityofpaclitaxelduetoitsinhibitoryeffectontheeffluxfunctionofABCB1,itenhancestheinhibitoryeffectofpaclitaxelonthegrowthofSW620/Ad300tumorandpromotedapoptosis[1].AnimalModel:5-10weekMaleathymicNCR(nu/nu)nudemiceABCB1overexpressingtumorxenograftmodelwithSW620/Ad300cellsDosage:30?mg/kgAdministration:Deliverorally;every3rdday;18daysResult:Leadtohigherintratumoralaccumulationofpaclitaxelintumors.REFERENCES[1].WangYJ,etal.Thiazole-valinepeptidomimetic(TTT-28)antagonizesmultidrugresistanceinvitroandinvivobyselectivelyinhibitingtheeffluxactivityofABCB1.SciRep.2017Feb9;7:42106.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications