Fedratinib-TG-101348-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEFedratinibCat.No.:HY-10409CASNo.:936091-26-8Synonyms:TG-101348;SAR302503分⼦式:C₂₇H₃₆N₆O₃S分⼦量:524.68作⽤靶点:JAK;Apoptosis作⽤通路:Epigenetics;JAK/STATSignaling;ProteinTyrosineKinase/RTK;StemCell/Wnt;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:125mg/mL(238.24mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.9059mL9.5296mL19.0592mL5mM0.3812mL1.9059mL3.8118mL10mM0.1906mL0.9530mL1.9059mL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)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(3.96mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(3.96mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.96mM);Clearsolution4.请依序添加每种溶剂：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥2.87mg/mL(5.47mM);Clearsolution5.请依序添加每种溶剂：5%DMSO>>95%(20%SBE-β-CDinsaline)Solubility:2.87mg/mL(5.47mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性Fedratinib(TG-101348)⼀种有效的，选择性的，ATP竞争性和具有⼝服活性的JAK2抑制剂，对于JAK2和JAK2V617F激酶的IC50均为3nM。Fedratinib对JAK2的选择性分别⽐JAK1和JAK3⾼35倍和334倍。Fedratinib可诱导癌细胞凋亡(apoptosis)，并可⽤于⾻髓增⽣性疾病的研究。IC50&TargetJAK2JAK2(V617F)Flt3Ret3nM(IC50)3nM(IC50)15nM(IC50)48nM(IC50)体外研究Fedratinib(TG101348)inhibitsproliferationofahumanerythroblastleukemia(HEL)celllinethatharborstheJAK2V617Fmutation,aswellasamurinepro-BcelllineexpressinghumanJAK2V617F(Ba/F3JAK2V617F),withanIC50valueofapproximately300nMforeitherline.ProliferationofparentalBa/F3cellswasinhibitedtoacomparablelevel,withanIC50valueof-420nM[1].ExposureofthesecellstoFedratinib(TG101348)(0.1μM,0.3μM,1μM,3μM,and10μM)reducesSTAT5phosphorylationatconcentrationsthatparalleltheconcentrationsrequiredtoinhibitcellproliferation[1].Fedratinib(TG101348)(0.1μM,0.3μM,1μM,3μM,and10μM)inducesapoptosisinbothHELandBa/F3JAK2V617Fcellsinadose-dependentmanner[1].体内研究Fedratinib(TG101348;60-120mg/kg;oralgavage;twicedaily;for42days;C57Bl/6mice)trewatmentshowsadose-dependentreductioninpolycythemiaandamarkeddose-dependentreductioninsplenomegalyoftreatedanimals[1].AnimalModel:C57Bl/6miceinducedbytheJAK2V617Fmutation[1]Dosage:60mg/kg,120mg/kgAdministration:Oralgavage;twicedaily;for42daysResult:Showedastatisticallysignificantreductioninhematocritandleukocytecount,adose-dependentreduction/eliminationofextramedullaryhematopoiesis.户使⽤本产品发表的科研⽂献2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•MolCancer.2021May29;20(1):80.•SignalTransductTargetTher.2022Feb23;7(1):52.•SignalTransductTargetTher.2020Dec26;5(1):295.•SciTranslMed.2018Jul18;10(450).pii:eaaq1093.•CellSyst.2018Apr25;6(4):424-443.e7.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].WernigG,etal.EfficacyofTG101348,aselectiveJAK2inhibitor,intreatmentofamurinemodelofJAK2V617F-inducedpolycythemiavera.CancerCell.2008Apr;13(4):311-20.[2].GeronI,etal.SelectiveinhibitionofJAK2-drivenerythroiddifferentiationofpolycythemiaveraprogenitors.CancerCell.2008Apr;13(4):321-30.McePdfHeightCaution: