Home JAK/STAT JAK inhibitor Upadacitinib For research use only.

Upadacitinib

Synonyms: ABT-494

Upadacitinib 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 Chemical Structure

Upadacitinib Chemical Structure

CAS: 1310726-60-3

Selleck's Upadacitinib has been cited by 9 publications

Purity & Quality Control

Batch: Purity: 99.99%
99.99

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Biological Activity

Description Upadacitinib 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
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
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].
Animal Research Animal Models Female Lewis rats
Dosages 10 mg/kg
Administration o.g.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05496348 Recruiting Ulcerative Colitis AbbVie October 20 2022 --
NCT05494606 Recruiting Ulcerative Colitis AbbVie August 15 2022 --
NCT05394792 Recruiting Atopic Dermatitis AbbVie June 1 2022 --
NCT05327920 Active not recruiting Rheumatoid Arthritis AbbVie April 20 2022 --
NCT05170646 Recruiting Rheumatoid Arthritis AbbVie March 14 2022 --
NCT05139836 Recruiting Atopic Dermatitis AbbVie December 13 2021 --

Chemical lnformation & Solubility

Molecular Weight 380.37 Formula

C17H19F3N6O
CAS No. 1310726-60-3 SDF --
Smiles CCC1CN(CC1C2=CN=C3N2C4=C(NC=C4)N=C3)C(=O)NCC(F)(F)F
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 76 mg/mL ( (199.8 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 76 mg/mL

Water : Insoluble


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In vivo
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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.
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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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