Gemcitabine-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemEGemcitabineCat.No.:HY-17026CASNo.:95058-81-4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(protectfromlight)溶解性数据体外实验DMSO:≥103.3mg/mL(392.48mM)扫描⼆维码，Ethanol:3.33mg/mL(12.65mM;Needultrasonic)运⽤溶解⽅案计算器*"≥"meanssoluble,butsaturationunknown.获得适合您实验体系的溶解⽅案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，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。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.请依序添加每种溶剂：1%DMSO99%saline2.Solubility:≥0.52mg/mL(1.98mM);Clearsolution请依序添加每种溶剂：10%DMSO40%PEG3005%Tween-8045%salineSolubility:2.08mg/mL(7.90mM);Suspendedsolution;Needultrasonic此⽅案可获得2.08mg/mL(7.90mM)的均匀悬浊液，悬浊液可⽤于⼝服和腹腔注射。1/3www.MedChemEwww.MedChemE以1mL⼯作液为例，取100μL20.8mg/mL的澄DMSO储备液加到400μLPEG300中，混合均匀；向上述3.体系中加⼊50μLTween-80，混合均匀；然后继续加⼊450μL⽣理盐⽔定容⾄1mL。请依序添加每种溶剂：10%DMSO90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(7.90mM);Clearsolution此⽅案可获得≥2.08mg/mL(7.90mM，饱和度未知)的澄溶液。以1mL⼯作液为例，取100μL20.8mg/mL的澄DMSO储备液加到900μL20%的SBE-β-CD⽣理盐⽔⽔溶4.液中，混合均匀。请依序添加每种溶剂：10%DMSO90%cornoilSolubility:≥2.08mg/mL(7.90mM);Clearsolution此⽅案可获得≥2.08mg/mL(7.90mM，饱和度未知)的澄溶液，此⽅案不适⽤于实验周期在半个⽉以上的实验。5.以1mL⼯作液为例，取100μL20.8mg/mL的澄DMSO储备液加到900μL⽟⽶油中，混合均匀。请依序添加每种溶剂：5%DMSO40%PEG3005%Tween-8050%saline6.Solubility:≥2.62mg/mL(9.95mM);Clearsolution请依序添加每种溶剂：5%DMSO95%(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,i.p.)orthecombinationDMAPT/Gemcitabinesignificantlyincreasesthemediansurvivaltimebymorethan30dayscomparedtotheplacebogroup(254.5or255daysvs.217.5days,respectively)[3].2/3www.MedChemEwww.MedChemE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.•SciTranslMed.2021Jan20;13(577):eaba7401.•Hepatology.2019May;69(5):1995-2012.•RedoxBiol.2020,101807.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):574-589.McePdfHeight关注MCE中国公众号，

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