Abrocitinib-PF-04965842-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAbrocitinibCat.No.:HY-107429CASNo.:1622902-68-4Synonyms:PF-04965842分⼦式:C₁₄H₂₁N₅O₂S分⼦量:323.41作⽤靶点:JAK作⽤通路:Epigenetics;JAK/STATSignaling;ProteinTyrosineKinase/RTK;StemCell/Wnt储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:125mg/mL(386.51mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.0921mL15.4603mL30.9205mL5mM0.6184mL3.0921mL6.1841mL10mM0.3092mL1.5460mL3.0921mL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)1/2MasterofBioactiveMolecules—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(6.43mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(6.43mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(6.43mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Abrocitinib(PF-04965842)⼀种有效、可⼝服、选择性的JAK1抑制剂，对JAK1和JAK2的IC50值分别为29和803nM。Abrocitinib(PF-04965842)可抑制TYK2的活性(IC50，1.253μM)和刺激后STAT1，STAT3和STAT5的磷酸化⽔平。可⽤于⾃⾝免疫症的研究[1]。IC50&TargetJAK1JAK2Tyk229nM(IC50)803nM(IC50)1253nM(IC50)体外研究Abrocitinib(Compound25)inhibitsIFNα-stimulatedphosphorylationofSTAT3,IFN-stimulatedphosphorylationofSTAT1inhumanwholeblood(HWB),aswellaspSTAT5inCD34+spikedintoHWB(JAK2),withIC50sof189,163nM,7.178μM,respectively[1].体内研究Abrocitinib(Compound25;5,15,50mg/kg,p.o.,dailyfor7days)significantlyreducespawswellinginratadjuvant-inducedarthritismodel[1].AnimalModel:FemaleLewisrats(8−10weeksold)[1]Dosage:5,15,50mg/kgAdministration:P.O.dailyfor7daysResult:Obviouslyreducedpawswellingatalldoses.户使⽤本产品发表的科研⽂献•IntJMolSci.2022Oct28;23(21):13122.•BioorgChem.6December2021,105538.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].VazquezML,etal.IdentificationofN-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide(PF-04965842):ASelectiveJAK1ClinicalCandidatefortheTreatmentofAutoimmuneDiseases.JMedChem.2018Feb8;61(3):1130-115McePdfHeight2/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECaution:Producthasnotbeenfullyvalidatedformedicalapplications