For research use only.
CAS No. 1310726-60-3
Upadacitinib (ABT-494) is a selective JAK1 inhibitor which demonstrates activity against JAK1 (0.045 μM) and JAK2 (0.109 μM), with > 40 fold selectivity over JAK3 (2.1 μM) and 100 fold selectivity over TYK2 (4.7 μM) as compared to JAK1.
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|Description||Upadacitinib (ABT-494) is a selective JAK1 inhibitor which demonstrates activity against JAK1 (0.045 μM) and JAK2 (0.109 μM), with > 40 fold selectivity over JAK3 (2.1 μM) and 100 fold selectivity over TYK2 (4.7 μM) as compared to JAK1.|
Upadacitinib is most potent on JAK1compared to other family members (JAK1 > JAK2 > JAK3 > TYK2). Upadacitinib demonstrates selectivity across a broad panel of 70+ kinases, with only Rock1 and Rock2 demonstrating IC50 values below 1 μM. Consistent with the Ba/F3 cellular data, upadacitinib potently inhibits the JAK1 dependent cytokines IL-6, OSM, IL-2, and IFNγ, as measured by inhibition of STAT phosphorylation.
|In vitro||DMSO||76 mg/mL (199.8 mM)|
|Ethanol||76 mg/mL (199.8 mM)|
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|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
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|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04758117||Recruiting||--||Psoriatic Arthritis||AbbVie||February 9 2021||--|
|NCT04541810||Recruiting||--||Rheumatoid Arthritis (RA)||AbbVie||January 26 2021||--|
|NCT04574492||Recruiting||--||Rheumatoid Arthritis (RA)||AbbVie||October 7 2020||--|
|NCT04497597||Recruiting||--||Rheumatoid Arthritis (RA)||AbbVie||October 16 2020||--|
|NCT01741493||Completed||Drug: ABT-494|Drug: Placebo|Drug: Tofacitinib||Rheumatoid Arthritis||AbbVie (prior sponsor Abbott)|AbbVie||November 2012||Phase 1|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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