Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPF-06843195Cat.No.:HY-131972CASNo.:2067281-51-8分?式:C??H??F?N?O?分?量:498.46作?靶點:PI3K作?通路:PI3K/Akt/mTOR儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數據體外實驗DMSO:62.5mg/mL(125.39mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.0062mL10.0309mL20.0618mL5mM0.4012mL2.0062mL4.0124mL10mM0.2006mL1.0031mL2.0062mL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:≥2.08mg/mL(4.17mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.17mM);ClearsolutionBIOLOGICALACTIVITY?物活性PF-06843195?種?度選擇性的PI3Kα抑制劑，在Rat1成纖維細胞中，其IC50為18nM。PF-06843195作?于PI3Kα和PI3Kδ的Ki分別?于0.018nM和0.28nM。PF-06843195對PI3K/mTOR信號通路有明顯抑制作?，且具有持久的抗腫瘤作?。IC50&TargetPI3KαPI3KβPI3KδPI3Kα18nM(IC50,inRat1360nM(IC50,inRat1160nM(IC50,inRat10.018nM(Ki)fibroblasts)fibroblasts)fibroblasts)PI3Kδ0.28nM(Ki)體外研究PF-06843195inhibitsthebreastcancercelllinesMCF7andT47DproliferationwithIC50sof62nMand32nM,respectively[1].PF-06843195inhibitspAKT(T308)inMCF7andT47DcellswithIC50sof7.8nMand8.7nM,respectively[1].體內研究Inrats,PF-06843195canrapidlyandquantitativelytransformfromPF-06862309[1].PF-06843195exhibitsoralbioavailability(rat25%)followingoraladministration(rat10mg/kg)[1].PF-06843195exhibitsamoderatehalf-life(rat3.6h)duetohighplasmaclearance(30mL/min/kg)combinedwithlargevolumesofdistribution(3.0L/kg)followingintravenousadministration(rat2mg/kg)[1].AnimalModel:MaleWistarHanRats[1]Dosage:2mg/kg(intravenous)and10mg/kg(oralgavage)(PharmacokineticAnalysis)Administration:Intravenous(IV)ororalgavage(PO)Result:T1/2of3.6hforrats.REFERENCES[1].HengmiaoCheng,etal.Structure-BasedDrugDesignandSynthesisofPI3Kα-SelectiveInhibitor(PF-06843195).JMedChem.2021Jan14;64(1):644-661.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forre