Upadacitinib (ABT-494)

For research use only.

Catalog No.S8162

3 publications

Upadacitinib (ABT-494) Chemical Structure

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.

Selleck's Upadacitinib (ABT-494) has been cited by 3 publications

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Biological Activity

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.
Targets
JAK1 [1]
(Cell-free assay)
JAK2 [1]
(Cell-free assay)
45 nM 109 nM
In vitro

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[1].

In vivo

Upadacitinib inhibits disease pathology in rat adjuvant induced arthritis[1]. It is a non-sensitive substrate for cytochrome P450, approximately 20% is eliminated, unchanged, in urine[2].

Protocol

Solubility (25°C)

In vitro DMSO 76 mg/mL (199.8 mM)
Ethanol 76 mg/mL (199.8 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 380.37
Formula

C17H19F3N6O

CAS No. 1310726-60-3
Storage powder
in solvent
Synonyms N/A
Smiles CCC1CN(CC1C2=CN=C3N2C4=C(NC=C4)N=C3)C(=O)NCC(F)(F)F

In vivo Formulation Calculator (Clear solution)

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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

Tech Support

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.

Handling Instructions

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JAK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID