PF-9363-CTx-648-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPF-9363Cat.No.:HY-132283CASNo.:2569009-58-9Synonyms:CTx-648分⼦式:C₂₀H₂₀N₄O₆S分⼦量:444.46作⽤靶点:HistoneAcetyltransferase作⽤通路:Epigenetics储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:250mg/mL(562.48mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.2499mL11.2496mL22.4992mL5mM0.4500mL2.2499mL4.4998mL10mM0.2250mL1.1250mL2.2499mL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%saline1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(4.68mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.08mg/mL(4.68mM);Suspendedsolution;Needultrasonic3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.68mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性PF-9363(CTx-648)⼀种⼀流⾼效、⾼选择性KAT6A/KAT6B抑制剂。PF-9363可⽤于癌症研究[1][2]。IC50&TargetKAT6A/KAT6B[1]体外研究PF-9363(0~1μM;1day;ZR75-1,T47DandMCF7cells)down-regulatestheexpressionofH3K23Acbiomarker[1].PF-9363leadstodownregulationofaspecificsetofgenesinvolvedinESR1pathway,cellcycleandstemcellpathways.PF-9363showsthattheIC50valuesforZR75-1andT47Dare0.3nMand0.9nM[1].WesternBlotAnalysis[1]CellLine:ZR75-1,T47DandMCF7cellsConcentration:0~1μMIncubationTime:1dayResult:Down-regulatedtheexpressionofH3K23Acbiomarker.体内研究PF-9363showsstronganti-tumoractivityinpatient-derivedxenograftmodels[1].REFERENCES[1].ShikharS,etal.First-in-classKAT6A/KAT6BInhibitorCTx-648(PF-9363)DemonstratesPotentAnti-tumorActivityinER+BreastCancerwithKAT6ADysregulation[2].WO2020254946McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.T