IITZ-01-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEIITZ-01Cat.No.:HY-112897CASNo.:1807988-47-1分⼦式:C₂₆H₂₃FN₈O分⼦量:482.51作⽤靶点:Autophagy;PI3K;Apoptosis作⽤通路:Autophagy;PI3K/Akt/mTOR;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:150mg/mL(310.87mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.0725mL10.3625mL20.7250mL5mM0.4145mL2.0725mL4.1450mL10mM0.2072mL1.0362mL2.0725mL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:≥2.5mg/mL(5.18mM);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:2.5mg/mL(5.18mM);Suspendedsolution;Needultrasonic3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.18mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性IITZ-01⼀个具有抗肿瘤活性的、有效的亲溶酶体的⾃噬抑制剂，其对PI3Kγ的IC50值为2.62μM。IC50&TargetPI3KγAutophagy2.62μM(IC50)体外研究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.体内研究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—您⾝边的抑制剂⼤师www.MedChemEcancerinvitroandinvivo.Oncogene.2018Aug30.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalappl