Upadacitinib

Catalog No.S8162 Batch:S816203

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Technical Data

Formula

C17H19F3N6O
Molecular Weight 380.37 CAS No. 1310726-60-3
Solubility (25°C)* In vitro DMSO 76 mg/mL (199.8 mM)
Ethanol 76 mg/mL (199.8 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
3.8mg/ml Taking the 1 mL working solution as an example, add 50 μL of clarified DMSO stock solution of 76 mg/ml to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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)

Animal Study:

[3]
  • Animal Models

    Female Lewis rats

  • Dosages

    10 mg/kg

  • Administration

    o.g.

Selleck's Upadacitinib has been cited by 10 publications

Type 1 interferons and Foxo1 down-regulation play a key role in age-related T-cell exhaustion in mice [ Nat Commun, 2024, 15(1):1718] PubMed: 38409097
Macrophage re-programming by JAK inhibitors relies on MAFB [ Cell Mol Life Sci, 2024, 81(1):152] PubMed: 38528207
IL-6 prevents Th2 cell polarization by promoting SOCS3-dependent suppression of IL-2 signaling [ Cell Mol Immunol, 2023, 10.1038/s41423-023-01012-1] PubMed: 37046042
Effect of JAK inhibitors on the three forms of bone damage in autoimmune arthritis: joint erosion, periarticular osteopenia, and systemic bone loss [ Inflamm Regen, 2023, 43(1):44] PubMed: 37726797
Effect of JAK inhibitors on the three forms of bone damage in autoimmune arthritis: joint erosion, periarticular osteopenia, and systemic bone loss [ Inflamm Regen, 2023, 43(1):44] PubMed: 37726797
Stress signalling and STAT1 activation characterize the keratinocytic gene expression pattern in Hidradenitis suppurativa [ J Eur Acad Dermatol Venereol, 2022, 36(12:2488-2498)] PubMed: 35881108
An epidermal keratinocyte homogenate induced type 2 and proinflammatory cytokine expression in cultured dermal cells [ J Dermatol Sci, 2022, S0923-1811(22)00092-5] PubMed: 35437207
Impact of Different JAK Inhibitors and Methotrexate on Lymphocyte Proliferation and DNA Damage [ J Clin Med, 2021, 10(7)1431] PubMed: 33916057
Janus kinase inhibitors ruxolitinib and baricitinib impair glycoprotein-VI mediated platelet function [ Platelets, 2021, 1-12] PubMed: 34097573
Emerging systemic JAK inhibitors in the treatment of atopic dermatitis: a review of abrocitinib, baricitinib, and upadacitinib [ Drugs Context, 2020, 92020-8-5] PubMed: 33240390

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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