CustomerValidation
- •CancerLett.2017Aug18;407:45-56.
- •CellDeathDis.2017Mar23;8(3):e2702.
- •JExpClinCancerRes.2017Oct19;36(1):149.
- •MolCarcinog.2017Mar;56(3):1082-1087.
| Description | ActinomycinDinhibitsDNArepairwithIC50of0.42μM. |
|---|---|
| IC50&Target | IC50:0.42μM(DNArepair)[1] |
| InVitro | ActinomycinDisaninhibitorofDNAtranscriptionandreplication[1].ActinomycinDmarkedlyreducesthevascularsmoothmusclecells(SMC)proliferationviatheinhibitionofBrdUincorporationat80nM.ThisisfurthersupportedbytheG1-phasearrestusingaflowcytometricanalysis.ActinomycinDisextremelypotentwithaninhibitoryconcentrationIC50at0.4nM,whereasthelethaldoseLD50isat260microM.Theproteinexpressionlevelsofproliferatingcellnuclearantigen(PCNA),focaladhesionkinase(FAK),andRafareallsuppressedbyActinomycinD.Extracellularsignal-regulatedkinases(Erk)involvedincell-cyclearrestarefoundtoincreasebyActinomycinD[2]. |
| InVivo | Thepluronicgelcontaining80nMand80μMActinomycinDisappliedtopicallytosurroundtheratcarotidadventitia,thethicknessofneointimaissubstantiallyreduced(45and55%,respectively)[2].MiceintheActinomycinDandfludarABInegrouplivessignificantlylongerthanthecontrolgroupwithPvaluesof<0.001 and="" 0.007,="" respectively.="" interestingly,="" single="" treatment="" with="" actinomycin="" d="" is="" superior="" to="" fludarabine="" regarding="" overall="" survival="" (p="">[3]. |
| ClinicalTrial | ViewMoreCollapse |
| References |
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| PreparingStockSolutions |
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent. | ||||||||||||||||
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| KinaseAssay [1] | ActinomycinDisco-incubatedfor3hat30°Cwithareactionmixturecontaining:120mgofawhole-cellextractofHeLacells,70mMKCl,0.4mMeachofdGTP,dCTP,dATP,anddigoxygenylated-dUTPinreactionbuffercontaining40mMHepes-KOH(pH7.6),5mMMgCl2,0.5mMDithiotreitol,2mMEGTA,10mMphosphocreatine,50mg/mLcreatinephosphate,and360mg/mLofbovineserumalbumin.Duringthisreaction,DNAdamageisrecognizedandtheexcisedpatchesarereplacedbyneosynthesizedDNAfragments.ThroughoutthisDNAsynthesis,digoxygenylated-dUMPsareincorporated.TheDNArepairreactionisstoppedbythreewashes[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly. | ||||||||||||||||
| AnimalAdmiNISTration [3] | ActinomycinDispreparedinphosphate-bufferedsaline(PBS)(Mice)[3]. Mice[3] | ||||||||||||||||
| References |
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| MolecularWeight | 1255.42 | ||||||||||||
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| Formula | C₆₂H₈₆N₁₂O₁₆ | ||||||||||||
| CASNo. | 50-76-0 | ||||||||||||
| Storage |
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| Shipping | RoomtemperatureincontinentalUS;mayvaryelsewhere | ||||||||||||
| Solvent&Solubility | DMSO:≥27mg/mL;DMSO:250mg/mL(Needultrasonic);Methanol:6.2mg/mL;Methanol:20mg/mL(Needultrasonic);H2O:<12.5=""> *"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation=""> Purity:99.89% |
