Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEGemcitabinehydrochlorideCat.No.:HY-B0003CASNo.:122111-03-9Synonyms:LY188011hydrochloride分?式:C?H??ClF?N?O?分?量:299.66作?靶點(diǎn):DNA/RNASynthesis;NucleosideAntimetabolite/Analog;Autophagy;Apoptosis作?通路:CellCycle/DNADamage;Autophagy;Apoptosis儲(chǔ)存?式:4°C,sealedstorage,awayfrommoistureandlight*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoistureandlight)溶解性數(shù)據(jù)體外實(shí)驗(yàn)H2O:33.33mg/mL(111.23mM;Needultrasonic)DMSO:25mg/mL(83.43mM;ultrasonicandwarmingandheatto60°C)DMF:2.5mg/mL(8.34mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM3.3371mL16.6856mL33.3712mL5mM0.6674mL3.3371mL6.6742mL10mM0.3337mL1.6686mL3.3371mL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；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoistureandlight)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(6.94mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(6.94mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(6.94mM);Clearsolution4.請(qǐng)依序添加每種溶劑：PBSSolubility:60mg/mL(200.23mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性GemcitabineHydrochloride(LY188011Hydrochloride)?種嘧啶核苷類似物抗代謝藥(nucleosideantimetabolite/analog)和抗腫瘤劑。Gemcitabine抑制DNA合成(DNAsynthesis)和修復(fù)，導(dǎo)致細(xì)胞?噬(autophagy)和凋亡(apoptosis)。IC50&TargetDNAsynthesis[1]體外研究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.體內(nèi)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].戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?Nature.2019Oct;574(7777):264-267.?CellRes.2020Jul;30(7):574-589.?AdvMater.2021May;33(18):e2100949.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師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