ETP-45658-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEETP-45658Cat.No.:HY-110109CASNo.:1198357-79-7分⼦式:C₁₆H₁₇N₅O₂分⼦量:311.34作⽤靶点:PI3K;DNA-PK;mTOR作⽤通路:PI3K/Akt/mTOR;CellCycle/DNADamage储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.溶解性数据体外实验DMSO:250mg/mL(802.98mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.2119mL16.0596mL32.1192mL5mM0.6424mL3.2119mL6.4238mL10mM0.3212mL1.6060mL3.2119mL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(6.68mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(6.68mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(6.68mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性ETP-45658⼀种有效的PI3K抑制剂，抑制PI3Kα，PI3Kδ，PI3Kβ和PI3Kγ的IC50值分别为22.0nM，39.8nM，129.0nM和717.3nM。ETP-45658还可以抑制DNA-PK(IC50=70.6nM)和mTOR(IC50=152.0nM)。ETP-45658可⽤于癌症研究。IC50&TargetPI3KαPI3KδPI3KβPI3Kγ22.0nM(IC50)39.8nM(IC50)129.0nM(IC50)717.3nM(IC50)mTORDNA-PK152.0nM(IC50)70.6nM(IC50)体外研究ETP-45658(10μM;4h)decreasesinthephosphorylationofFOXO3a,Gsk3-βandp70S6KinU2OScells[1].ETP-45658inhibitstheproliferationofMCF7,PC3,786-O,HTC116,andU251cells,withEC50sof0.48μM,0.49μM,2.62μM,3.53μM,and5.56μM,respectively[1].ETP-45658(10μM;24h)inducesaclearG1arrestofPC3cells[1].ETP-45658inhibitsthemutantPI3Kαproteins,H1047RandE545K,withIC50sof16.8nMand13.1nM,respectively[1].ETP-45658(5nM-11.1μM;1h)inducesadose-dependentincreaseofGFP-FOXOnucleartranslocationinU2foxRELOCcells[1].ETP-45658(10μM;1h)decreasetheexpressionofcyclinD1andp-Aktonserine473inU2OScells[1].WesternBlotAnalysis[1]CellLine:U2OScellsConcentration:10μMIncubationTime:4hoursResult:Causeda95%decreaseinthephosphorylationofFOXO3aatthreonine32anda55%reductiononGsk3-βatserine9.ReducedthephosphorylationofthemTORsubstratep70S6K.体内研究ETP-45658(22.7mg/kg)decreasesthelevelofphosphorylatedAktonserine473inthemammaryductsoftransgenicmice[1].REFERENCES[1].LinkW,et,al.ChemicalinterrogationofFOXO3anucleartranslocationidentifiespotentandselectiveinhibitorsofphosphoinositide3-kinases.JBiolChem.2009Oct9;284(41):28392-28400.[2].HillR,et,al.Anovelphosphatidylinositol3-kinase(PI3K)inhibitordirectsapotentFOXO-dependent,p53-independentcellcyclearrestphenotypecharacterizedbythedifferentialinductionofasubsetofFOXO-regulatedgenes.BreastCancerRes.2014Dec9;16(6):482.McePdfHeight2/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECaution:Producthasnotbeenfullyvalidatedfo