Tefinostat-CHR-2845-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemETefinostatCat.No.:HY-106409CASNo.:914382-60-8Synonyms:CHR-2845分⼦式:C₂₈H₃₇N₃O₅分⼦量:495.61作⽤靶点:HDAC;Apoptosis作⽤通路:CellCycle/DNADamage;Epigenetics;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(201.77mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.0177mL10.0886mL20.1772mL5mM0.4035mL2.0177mL4.0354mL10mM0.2018mL1.0089mL2.0177mL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:≥2.5mg/mL(5.04mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.04mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥0.83mg/mL(1.67mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Tefinostat(CHR-2845)⼀种单核细胞/巨噬细胞靶向组蛋⽩脱⼄酰酶(HDAC)抑制剂。Tefinostat可被胞内酯酶⼈羧酸酯酶-1(hCE-1)裂解成活性酸CHR-2847。Tefinostat可⽤于⽩⾎病的研究。IC50&TargetHDAC体外研究Tefinostat(CHR-2845)(1-4nM)hasefficacyinAMLcelllinesHL60(M2FABtype),MV411(M4,FLT3-ITD),OCIAML3(M4NPM1mut)andTHP1(M5)withEC50valuesof2.3μM,57nM,110nMand560nM,respectively[1].Tefinostat(0,0.5,1and5μM;24,48h)hasdose-dependentinductionofapoptosisandsignificantgrowthinhibitoryeffects[1].CellViabilityAssay[1]CellLine:AMLcelllinesConcentration:1-4nMIncubationTime:Result:Hadsignificantgrowthinhibitoryeffects.ApoptosisAnalysis[1]CellLine:myelo-monocyticcelllinesandHL60cellsConcentration:0,0.5,1and5μMIncubationTime:24,48hResult:Showedstrongapoptoticinductioninmyelo-monocyticcelllinesTHP1,MV411(FLT3-ITD)andOCIAML3within24hoursandonlyreachedinnonmonocyticHL60cellsatmuchhigherconcentrations.REFERENCES[1].ZabkiewiczJ,etal.Thetargetedhistonedeacetylaseinhibitortefinostat(CHR-2845)showsselectiveinvitroefficacyinmonocytoid-lineageleukaemias.Oncotarget.2016Mar29;7(13):16650-62.McePdfHeight2/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forr