Upadacitinib (ABT-494)

製品コードS8162 バッチS816201

印刷

化学情報

Synonyms

ABT-494

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₁₇H₁₉F₃N₆O

分子量

380.37

CAS No.

1310726-60-3

Solubility (25°C)*

体外

DMSO

76 mg/mL (199.8 mM)

Ethanol

76 mg/mL (199.8 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	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.
in vitro	Upadacitinib is most potent on JAK1compared to other family members (JAK1 > JAK2 > JAK3 > TYK2). This compound 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, it 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]. This compound is a non-sensitive substrate for cytochrome P450, approximately 20% is eliminated, unchanged, in urine^[2].

製品説明

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.

in vitro

Upadacitinib is most potent on JAK1compared to other family members (JAK1 > JAK2 > JAK3 > TYK2). This compound 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, it 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].

This compound is a non-sensitive substrate for cytochrome P450, approximately 20% is eliminated, unchanged, in urine^[2].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	NK cells
	濃度	JAK1 (0.045 μM) and JAK2 (0.109 μM)
	反応時間
	実験の流れ
動物実験	動物モデル	Female Lewis rats
	投薬量	10 mg/kg
	投与方法	o.g.

参考

https://bmcrheumatol.biomedcentral.com/articles/10.1186/s41927-018-0031-x
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6425155/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Differential effects of tofacitinib on macrophage activation contribute to lack of response in ulcerative colitis patients [ J Crohns Colitis, 2025, 19(6)jjaf076]	PubMed: 40320713
Spatial proteomics identifies JAKi as treatment for a lethal skin disease [ Nature, 2024, ]	PubMed: 39415009
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
Loss of OVOL2 in Triple-Negative Breast Cancer Promotes Fatty Acid Oxidation Fueling Stemness Characteristics [ Adv Sci (Weinh), 2024, 11(24):e2308945]	PubMed: 38627980
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
IL-6 prevents Th2 cell polarization by promoting SOCS3-dependent suppression of IL-2 signaling [ Cell Mol Immunol, 2023, 20(6):651-665]	PubMed: 37046042
IL-6 prevents Th2 cell polarization by promoting SOCS3-dependent suppression of IL-2 signaling [ Cell Mol Immunol, 2023, 20(6):651-665]	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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。