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ABT-494 (Upadacitinib) JAK1 inhibitor

Cat.No.S8162

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.
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Quality Control

Batch: Purity: 99.99%
99.99
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Solubility in DMSO or Water

In vitro
Batch:

DMSO : 76 mg/mL (199.8 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 76 mg/mL

Water : Insoluble

The solubility data above are all experimental results (not literature values).

Molarity Calculator

Mass Concentration Volume Molecular Weight
Dilution Calculator Molecular Weight Calculator

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

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Calculation results:

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.

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Working Concentrations for Cell Culture Treatment

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Selectivity & Specificity

ABT-494 (Upadacitinib) is a potent inhibitor of JAK1 (0.76/40/43 nM), JAK2 (19/120 nM), JAK3 (224/2300 nM), TYK2 (118/4700 nM). ABT-494 (Upadacitinib) exhibits the greatest inhibitory potency toward JAK1 (IC50 = 0.76 nM).

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Mechanism of Action

Information Upadacitinib is a potent, selective, reversible, ATP-competitive JAK1 inhibitor. It affects JAK/STAT and NF-κB signaling pathways by binding to the kinase catalytic domain and blocking STAT phosphorylation, effectively inhibiting inflammatory responses and cytokine production.

Read more about ABT-494 (Upadacitinib) IC50 for cell-based and cell-free assays

Primary Applications and Mechanism of Action

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Chemical Information, Storage & Stability

Molecular Weight 380.37 Formula

C17H19F3N6O

Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1310726-60-3 -- Storage of Stock Solutions

Synonyms ABT-494 Smiles CCC1CN(CC1C2=CN=C3N2C4=C(NC=C4)N=C3)C(=O)NCC(F)(F)F

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