Gemcitabine-LY-188011-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEGemcitabineCat.No.:HY-17026CASNo.:95058-81-4Synonyms:LY188011分⼦式:C₉H₁₁F₂N₃O₄分⼦量:263.2作⽤靶点:NucleosideAntimetabolite/Analog;DNA/RNASynthesis;Autophagy;Apoptosis作⽤通路:CellCycle/DNADamage;Autophagy;Apoptosis储存⽅式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性数据体外实验DMSO:250mg/mL(949.85mM;Needultrasonic)Ethanol:12.5mg/mL(47.49mM;Needultrasonic)H2O:6.25mg/mL(23.75mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.7994mL18.9970mL37.9939mL5mM0.7599mL3.7994mL7.5988mL10mM0.3799mL1.8997mL3.7994mL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；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month(protectfromlight)。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。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。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：0.5%HPMC>>1%Tween80Solubility:20mg/mL(75.99mM);Clearsolution;Needultrasonic2.请依序添加每种溶剂：1%DMSO>>99%salineSolubility:≥0.52mg/mL(1.98mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(7.90mM);Clearsolution4.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(7.90mM);Clearsolution5.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.58mg/mL(9.80mM);Clearsolution6.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(7.90mM);Clearsolution7.请依序添加每种溶剂：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥2.62mg/mL(9.95mM);Clearsolution8.请依序添加每种溶剂：5%DMSO>>95%(20%SBE-β-CDinsaline)Solubility:≥2.62mg/mL(9.95mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Gemcitabine(LY188011)⼀种嘧啶核苷类似物抗代谢药(nucleosideantimetabolite/analog)和抗肿瘤剂。Gemcitabine抑制DNA合成(DNAsynthesis)和修复，导致细胞⾃噬(autophagy)和凋亡(apoptosis)[1][2]。IC50&TargetDNAsynthesis[1]体外研究Gemcitabine(purchasedfromMedChemExpress,0.003-1μM;3days)killsbothmouseandhumansenescentcellseffectivelyandpotently[4].GemcitabineinhibitsthegrowthofBxPC-3,MiaPaca-2,PANC-1,PL-45andAsPC-1cellswithIC50sof37.6,42.9,92.7,89.3and131.4nM,respectively[1].CellViabilityAssay[4]CellLine:Non-senescentandreplication-inducedsenescentnewborndermalfibroblasts(NBFs)Concentration:0.003,0.01,0.03,0.1,0.3,1μMIncubationTime:3daysResult:Killedreplication-inducedsenescentNBFsfor3dayswith11.0%cellviability.体内研究Gemcitabinecanbeadministeredviaendotrachealsprayinratswithoutmarkedtoxicitywithamaximumtolerateddoseof4mg/kgonceaweekfor9weeks.ThetoxicityofGemcitabineislowervialungthanoraladministrationatdosagesof2,4,and6mg/kg[2].TreatmentoftheLSL-KrasG12D/+;LSL-Trp53R172H;Pdx-1-CremicewitheitherGemcitabine(50mg/kg,2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEi.p.)orthecombinationDMAPT/Gemcitabinesignificantlyincreasesthemediansurvivaltimebymorethan30dayscomparedtotheplacebogroup(254.5or255daysvs.217.5days,respectively)[3].户使⽤本产品发表的科研⽂献•Nature.2019Oct;574(7777):264-267.•CellRes.2020Jul;30(7):574-589.•AdvMater.2021May;33(18):e2100949.•Gastroenterology.2021Nov;161(5):1601-1614.e23.•SciTranslMed.2021Jan20;13(577):eaba7401.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].WangH,etal.EnhancedefficacyofGemcitabinebyindole-3-carbinolinpancreaticcelllines:theroleofhumanequilibrativenucleosidetransporter1.AnticancerRes.2011Oct;31(10):3171-80.[2].Yip-SchneiderMT,etal.DimethylaminoparthenolideandGemcitabine:asurvivalstudyusingageneticallyengineeredmousemodelofpancreaticcancer.BMCCancer.2013Apr17;13:194.[3].GagnadouxF,etal.Safetyofpulmonaryadministrationofgemcitabineinrats.JAerosolMed.2005Summer;18(2):198-206[4].YushengCai,etal.Eliminationofsenescentcellsbyβ-galactosidase-targetedprodrugattenuatesinflammationandrestoresphysicalfunctioninagedmice.CellRes.2020Jul;30(7):574