PI-273-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPI-273Cat.No.:HY-103489CASNo.:925069-34-7分⼦式:C₁₆H₁₆ClN₃O₂S₂分⼦量:381.9作⽤靶点:PI4K;Apoptosis作⽤通路: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:6.02mg/mL(15.76mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.6185mL13.0924mL26.1849mL5mM0.5237mL2.6185mL5.2370mL10mM0.2618mL1.3092mL2.6185mL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。BIOLOGICALACTIVITY⽣物活性PI-273第⼀种可逆的和特异性磷脂酰肌醇4-激酶(PI4KIIα)抑制剂，IC50为0.47μM。PI-273可以抑制乳腺癌细胞的增殖，阻断细胞周期并诱导细胞凋亡。IC50&TargetPI4KIIα0.47μM(IC50)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE体外研究PI-273(2μM;48hours)blocksthecellcycleattheG2-Mphase[1].PI-273(2μM;48hours)inducescellapoptosisinallthreeRaswild-typebreastcancercells:MCF-7,T-47D,andSK-BR-3[1].PI-273(0.5-2μM;for3days)cansuppresstheAKTsignalingpathwayinadose-andtime-dependentmanner[1].PI-273of1μMand2μMinhibitsthecellproliferationofbothMCF-7andT-47Dcellsinatime-dependentmanner[1].CellCycleAnalysis[1]CellLine:MCF-7,T-47D,SK-BR-3,MDA-MB-231,SUM229PE,Hs578TcellsConcentration:2μMIncubationTime:48hoursResult:BlockedthecellcycleattheG2-Mphase.ApoptosisAnalysis[1]CellLine:MCF-7,T-47D,andSK-BR-3cellsConcentration:2μMIncubationTime:48hoursResult:InducedcellapoptosisinallthreeRaswild-typebreastcancercells:MCF-7,T-47D,andSK-BR-3.WesternBlotAnalysis[1]CellLine:MCF-7cellsConcentration:0.5,1,2μMIncubationTime:For3daysResult:SuppressedtheAKTsignalingpathwayinadose-andtime-dependentmanner.体内研究PI-273(intraperitonealinjection;25mg/kg/day;15days)profoundlysuppressesthetumorvolumeandweightintheMCF-7xenografts[1].PI-273(0.5mg/kg(intravenously)or1.5mg/kg(intragastrically);0.08-5hours)hasahalf-lifeof0.411hoursforintravenousadministrationand1.321hoursforintragastricaladministration,andtheabsolutebioavailabilityofPI-273is5.1%[1].AnimalModel:Eight-week-oldmaleBALB/cnudemicewithMCF-7cell[1]Dosage:25mg/kg2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAdministration:Intraperitonealinjection;daily;15daysResult:SuppressedthetumorvolumeandweightintheMCF-7xenografts.AnimalModel:MaleSprague-Dawley(SD)rats[1]Dosage:0.5mg/kg(intravenously)or1.5mg/kg(intragastrically)(PharmacokineticStudy)Administration:Intravenouslyorintragastrically;0.08,0.16,0.33,0.67,1,1.5,2,3and5hoursResult:Hasahalf-lifeof0.411hoursforintravenousadministrationand1.321hoursforintragastricaladministration,andtheabsolutebioavailabilityofPI-273is5.1%.REFERENCES[1].LiJ,etal.PI-273,aSubstrate-Competitive,SpecificSmall-MoleculeInhibitorofPI4KIIα,InhibitstheGrowthofBreastCancerCells.CancerRes.2017Nov15;77(22):6253-6266.McePdfHeightCaution:Producthasnotbeenfullyvalidat