Etoposide-phosphate-BMY-40481-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemEEtoposidephosphateCat.No.:HY-13630CASNo.:117091-64-2Synonyms:BMY-40481分?式:C??H??O??P分?量:668.54作?靶點(diǎn):Topoisomerase;Bacterial;Autophagy;Apoptosis作?通路:CellCycle/DNADamage;Anti-infection;Autophagy;Apoptosis儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCOA.溶解性數(shù)據(jù)體外實(shí)驗(yàn)H2O:125mg/mL(186.97mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.4958mL7.4790mL14.9580mL5mM0.2992mL1.4958mL2.9916mL10mM0.1496mL0.7479mL1.4958mL請(qǐng)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(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存?式和期限。BIOLOGICALACTIVITY?物活性Etoposidephosphate(BMY-40481)?種有效的抗癌(anti-cancer)化療試劑和?種選擇性拓?fù)洚悩?gòu)酶II(topoisomeraseII)抑制劑，可以防?DNA鏈的重新連接。Etoposidephosphate依托泊苷的磷酸酯前藥，被認(rèn)為與Etoposide活性相當(dāng)。Etoposidephosphate誘導(dǎo)細(xì)胞周期阻滯、凋亡(apoptosis)和?噬(autophagy)。IC50&TargetTopoisomeraseII體外研究Etoposidephosphateisawater-solublederivativeandprobableprodrugofetoposidecharacterizedbythe1/3MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemEpresenceofaphosphategroupinposition4'oftheEringoftheetoposidemolecule[1].Etoposidephosphate(0-1μM;72hours)inhibitsHCT116FBXW+/+,FBXW-/-andp53-/-asadose-dependentmanner,exhibitsIC50valuesof0.945μM;0.375μM;and1.437μM,respectively[2].Etoposidephosphate(25μM;6hours)delaysp53recoverinFBXW7-deficientcells.Inaddition,FBXW7expressionisdisappearedinFBXW7-/-cells[2].CellViabilityAssay[2]CellLine:FBXW+/+,FBXW-/-andp53-/-cellConcentration:0.025μM,0.05μM,0.075μM,0.1μM,0.2μM,0.4μM,0.6μM,0.8μM,1μMIncubationTime:72hoursResult:InhibitedHCT116FBXW+/+,FBXW-/-andp53-/-cellgrowthasaconcentrationmanner.WesternBlotAnalysis[2]CellLine:HCT116FBXW7+/+orFBXW7-/-cellsConcentration:25μMIncubationTime:6hoursResult:Exhibitedthattherecoveryofp53levelsafterDNAdamageismediatedbyFBXW7.體內(nèi)研究Etoposidephosphate(intravenousinjection;50,100,or150mg/kg;singledose)hasclinicalsymptomologyofprogressiveataxia,impairedrightingreflex,andsplayingandparesisoffore-andhindlimbsatday8infemaleCD-1mice[3].AnimalModel:FemaleCD-1mice[3]Dosage:50,100,or150mg/kgAdministration:Intravenousinjection;singledoseResult:Observeddegenerationofdorsalrootganglioncellsandaxonaldegenerationoftheirdistalandproximalprocessesinperipheralnerves,dorsalspinalroots,anddorsalfuniculiofthespinalcordatalldosesunderlightmicroscopy(LM).?AdvSci.2020Sep28.?Hepatology.2020May;71(5):1660-1677.?Hepatology.2020May;71(5):1660-1677.?EMBOMolMed.2020Oct7;e12525.?CellSyst.2019Jul24;9(1):35-48.e5.2/3MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemESeemorecustomervalidationsonwww.MedChemEREFERENCES[1].WitterlandAH,etal.Etoposidephosphate,thewatersolubleprodrugofetoposide.PharmWorldSci.1996Oct;18(5):163-70.[2].BregmanCL,etal.Etoposide-andBMY-40481-inducedsensoryneuropathyinmice.ToxicolPathol.1994Sep-Oct;22(5):528-35.[3].CuiD,etal.FBXW7ConfersRadiationSurvivalbyTargetingp53forDegradation.CellRep.2020Jan14;30(2):497-509.e4.[4].SUMMARYOFPRODUCTCHARACTERISTICSMcePdfHeightCaution:Producthasnotbeenfu