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Technical Data
| Formula | C17H19F3N6O |
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| 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 | |||
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* <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.) |
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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. | ||||
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| Targets |
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| 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]. |
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| 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: |
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References
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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 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
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.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.