CA-5f-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemECA-5fCat.No.:HY-112698CASNo.:1370032-19-1分⼦式:C₂₄H₂₄N₂O₃分⼦量:388.46作⽤靶点:Autophagy;Apoptosis作⽤通路:Autophagy;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:77.5mg/mL(199.51mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.5743mL12.8713mL25.7427mL5mM0.5149mL2.5743mL5.1485mL10mM0.2574mL1.2871mL2.5743mL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。-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.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(5.35mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.08mg/mL(5.35mM);Suspendedsolution;Needultrasonic3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.35mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性CA-5f⼀种有效的晚期巨⾃噬/⾃噬(macroautophagy/autophagy)抑制剂，通过抑制⾃噬体-溶酶体融合起作⽤。CA-5f能够增加LC3B-II(⼀种监控⾃噬的标记物)和SQSTM1蛋⽩⽔平，促进ROS的产⽣。具有抗肿瘤活性[1]。IC50&TargetMacroautophagy/autophagy[1]体外研究CA-5f(0-40μM,6hour)concentration-andtime-dependentlyelevatesthelevelofLC3B-II(amarkertomonitorautophagy)andSQSTM1proteinbothinA549cellsandHUVECs[1].CA-5f(20μM,6hours)inhibitsthedegradationofautophagosomeswhentreatedaloneorincombinationBafilomycinA1(100nM)orChloroquine(30μM)inA549cellsandHUVECs[1].CA-5f(20μM)neitherimpairsthehydrolyticfunctionnorthequantityoflysosomes[1].CA-5f(20μM,96hours)inhibitsthegrowthofA549cells,andlesscytotoxictonormalHUVECs[1].CellViabilityAssay[1]CellLine:A549,HUVECsConcentration:20μMIncubationTime:96hoursResult:ExhibitedmorecytotoxicityagainstA549cellscomparedwithnormalHUVECs.WesternBlotAnalysis[1]CellLine:A549cellsandHUVECsConcentration:0-40μMIncubationTime:6hoursResult:ElevatedLC3B-II(amarkertomonitorautophagy)andSQSTM1proteinlevelsinaconcentration-andtime-dependentmanner.体内研究CA-5f(40mg/kg,i.p.,every2daysforupto30days)iswelltolerated,andpotentlyinhibitsthegrowthoftumorinnudemicebearingA549lungcancercells[1].CA-5f(40mg/kg,i.p.)suppressesautophagicfluxandinducesapoptosisinnudemicebearingA549lungcancercells[1].2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAnimalModel:NudemicebearingA549lungcancercells[1]Dosage:40mg/kgAdministration:Injectedviacaudalvein,every2daysforupto30daysResult:Significantlysuppressedtumorvolumeandweightinmice,increasedthenumberofapoptoticcellsinmice.REFERENCES[1].ZhangL,etal.IdentificationofcompoundCA-5fasanovellate-stageautophagyinhibitorwithpotentanti-tumoreffectagainstnon-smallcelllungcancer.Autophagy.2019Mar;15(3):391-406.McePdfHeightCaution:Producthasnotbeenfullyvalid