Upadacitinib (ABT-494)

Catalog No.S8162

For research use only.

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 (ABT-494) Chemical Structure

CAS No. 1310726-60-3

Selleck's Upadacitinib (ABT-494) has been cited by 4 Publications

Purity & Quality Control

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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 (from reference)

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 380.37
Formula

C17H19F3N6O

CAS No. 1310726-60-3
Storage 3 years -20°C powder
2 years -80°C in solvent
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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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05170646 Not yet recruiting -- Rheumatoid Arthritis AbbVie January 28 2022 --
NCT05139836 Recruiting -- Atopic Dermatitis AbbVie December 13 2021 --
NCT05081557 Recruiting -- Atopic Dermatitis AbbVie October 19 2021 --
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 --

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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