PI-273-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPI-273Cat.No.:HY-103489CASNo.:925069-34-7分?式:C??H??ClN?O?S?分?量:381.9作?靶點(diǎn):PI4K;Apoptosis作?通路:PI3K/Akt/mTOR;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:6.02mg/mL(15.76mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.6185mL13.0924mL26.1849mL5mM0.5237mL2.6185mL5.2370mL10mM0.2618mL1.3092mL2.6185mL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?。BIOLOGICALACTIVITY?物活性PI-273第?種可逆的和特異性磷脂酰肌醇4-激酶(PI4KIIα)抑制劑，IC50為0.47μM。PI-273可以抑制乳腺癌細(xì)胞的增殖，阻斷細(xì)胞周期并誘導(dǎo)細(xì)胞凋亡。IC50&TargetPI4KIIα0.47μM(IC50)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE體外研究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.體內(nèi)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?邊的抑制劑?師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