IITZ-01-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEIITZ-01Cat.No.:HY-112897CASNo.:1807988-47-1分?式:C??H??FN?O分?量:482.51作?靶點:Autophagy;PI3K;Apoptosis作?通路:Autophagy;PI3K/Akt/mTOR;Apoptosis儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數據體外實驗DMSO:150mg/mL(310.87mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.0725mL10.3625mL20.7250mL5mM0.4145mL2.0725mL4.1450mL10mM0.2072mL1.0362mL2.0725mL請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據您的實驗動物和給藥?式選擇適當的溶解?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結果的可靠性，澄的儲備液可以根據儲存條件，適當保存；體內實驗的?作液，建議您現?現配，當天使?；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?；如在配制過程中出現沉淀、析出現象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(5.18mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(5.18mM);Suspendedsolution;Needultrasonic3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.18mM);ClearsolutionBIOLOGICALACTIVITY?物活性IITZ-01?個具有抗腫瘤活性的、有效的親溶酶體的?噬抑制劑，其對PI3Kγ的IC50值為2.62μM。IC50&TargetPI3KγAutophagy2.62μM(IC50)體外研究IITZ-01(0-2μM,24h)enhancesautophagosomesformationasindicatedbyincreasedexpressionofLC3-IIlevelstime-anddose-dependentlyintriple-negativebreastcancer(TNBC)celllines(MDA-MB-231andMDA-MB-453).IITZ-01alsodemonstratespotentautophagyinhibitoryactivityinotherbreast,lung,andcoloncancercells[1].WesternBlotAnalysis[1]CellLine:Triple-negativebreastcancer(TNBC)celllines(MDA-MB-231andMDA-MB-453).Concentration:0-2μM.IncubationTime:24hours.Result:EnhancedautophagosomesformationasindicatedbyincreasedexpressionofLC3-IIlevels.體內研究IITZ-01(45mg/kg,i.p.everyalternatedayfor4weeks)inhibitsaveragebreasttumorgrowthwhencomparedwithcontrolfromthirddayoftreatmentintriple-negativebreasttumormodelsinmice[1].AnimalModel:MDA-MB-231(TNBC)/greenfluorescentprotein(GFP)orthotropicbreastcancerxenograftsweredevelopedinCrTac:NCr-FoxnnuBALB/cfemalenudemice[1].Dosage:45mg/kg.Administration:Intraperitonealeveryalternatedayfor4weeks.Result:Inhibitedaveragebreasttumorgrowthwhencomparedwithcontrolfromthirddayoftreatment.REFERENCES[1].GuntukuL,etal.IITZ-01,anovelpotentlysosomotropicautophagyinhibitor,hassingle-agentantitumorefficacyintriple-negativebreast2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEcancerinvitroandinvivo.Oncogene.2018Aug30.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalappl