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

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEGemcitabinehydrochlorideCat.No.:HY-B0003CASNo.:122111-03-9Synonyms:LY188011hydrochloride分⼦式:C₉H₁₂ClF₂N₃O₄分⼦量:299.66作⽤靶点:DNA/RNASynthesis;NucleosideAntimetabolite/Analog;Autophagy;Apoptosis作⽤通路:CellCycle/DNADamage;Autophagy;Apoptosis储存⽅式:4°C,sealedstorage,awayfrommoistureandlight*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoistureandlight)溶解性数据体外实验H2O:33.33mg/mL(111.23mM;Needultrasonic)DMSO:25mg/mL(83.43mM;ultrasonicandwarmingandheatto60°C)DMF:2.5mg/mL(8.34mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.3371mL16.6856mL33.3712mL5mM0.6674mL3.3371mL6.6742mL10mM0.3337mL1.6686mL3.3371mL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(sealedstorage,awayfrommoistureandlight)。-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：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(6.94mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(6.94mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(6.94mM);Clearsolution4.请依序添加每种溶剂：PBSSolubility:60mg/mL(200.23mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性GemcitabineHydrochloride(LY188011Hydrochloride)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)。IC50&TargetDNAsynthesis[1]体外研究GemcitabineHydrochloride(purchasedfromMedChemExpress,0.003-1μM;3days)killsbothmouseandhumansenescentcellseffectivelyandpotently[4].GemcitabineHydrochlorideinhibitsthegrowthofBxPC-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GemcitabineHydrochloridecanbeadministeredviaendotrachealsprayinratswithoutmarkedtoxicitywithamaximumtolerateddoseof4mg/kgonceaweekfor9weeks.ThetoxicityofGemcitabineislowervialungthanoraladministrationatdosagesof2,4,and6mg/kg[2].TreatmentoftheLSL-KrasG12D/+;LSL-Trp53R172H;Pdx-1-CremicewitheitherGemcitabine(50mg/kg,i.p.)orthecombinationDMAPT/GemcitabineHydrochloridesignificantlyincreasesthemediansurvivaltimebymorethan30dayscomparedtotheplacebogroup(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):e2100949.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•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].GagnadouxF,etal.Safetyofpulmonaryadministrationofgemcitabineinrats.JAerosolMed.2005Summer;18(2):198-206[3].LouM,etal.Physicalinteractionbetweenhumanribonucleotidereductaselargesubunitandthioredoxinincreasescolorectalcancermalignancy.JBiolChem.2017Jun2;292(22):9136-9149.[4].Yip-SchneiderMT,etal.DimethylaminoparthenolideandGemcitabine:asurvivalstudyusingageneticallyengineeredmousemodelofpancreaticcancer.BMCCancer.2013Apr17;13:194.McePdfH