Abrocitinib-PF-04965842-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEAbrocitinibCat.No.:HY-107429CASNo.:1622902-68-4Synonyms:PF-04965842分?式:C??H??N?O?S分?量:323.41作?靶點(diǎn):JAK作?通路:Epigenetics;JAK/STATSignaling;ProteinTyrosineKinase/RTK;StemCell/Wnt儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:125mg/mL(386.51mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM3.0921mL15.4603mL30.9205mL5mM0.6184mL3.0921mL6.1841mL10mM0.3092mL1.5460mL3.0921mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(6.43mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(6.43mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(6.43mM);ClearsolutionBIOLOGICALACTIVITY?物活性Abrocitinib(PF-04965842)?種有效、可?服、選擇性的JAK1抑制劑，對(duì)JAK1和JAK2的IC50值分別為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?平?？?于??免疫癥的研究[1]。IC50&TargetJAK1JAK2Tyk229nM(IC50)803nM(IC50)1253nM(IC50)體外研究Abrocitinib(Compound25)inhibitsIFNα-stimulatedphosphorylationofSTAT3,IFN-stimulatedphosphorylationofSTAT1inhumanwholeblood(HWB),aswellaspSTAT5inCD34+spikedintoHWB(JAK2),withIC50sof189,163nM,7.178μM,respectively[1].體內(nèi)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.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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?邊的抑制劑?師www.MedChemECaution:Producthasnotbeenfullyvalidatedformedicalapplications