Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemECA-5fCat.No.:HY-112698CASNo.:1370032-19-1分?式:C??H??N?O?分?量:388.46作?靶點(diǎn):Autophagy;Apoptosis作?通路:Autophagy;Apoptosis儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:77.5mg/mL(199.51mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.5743mL12.8713mL25.7427mL5mM0.5149mL2.5743mL5.1485mL10mM0.2574mL1.2871mL2.5743mL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。-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.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(5.35mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.08mg/mL(5.35mM);Suspendedsolution;Needultrasonic3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.35mM);ClearsolutionBIOLOGICALACTIVITY?物活性CA-5f?種有效的晚期巨?噬/?噬(macroautophagy/autophagy)抑制劑，通過(guò)抑制?噬體-溶酶體融合起作?。CA-5f能夠增加LC3B-II(?種監(jiān)控?噬的標(biāo)記物)和SQSTM1蛋??平，促進(jìn)ROS的產(chǎn)?。具有抗腫瘤活性[1]。IC50&TargetMacroautophagy/autophagy[1]體外研究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.體內(nèi)研究CA-5f(40mg/kg,i.p.,every2daysforupto30days)iswelltolerated,andpotentlyinhibitsthegrowthoftumorinnudemicebearingA549lungcancercells[1].CA-5f(40mg/kg,i.p.)suppressesautophagicfluxandinducesapoptosisinnudemicebearingA549lungcancercells[1].2/3MasterofBioactiveMolecules—您?邊的抑制劑?師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