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Upadacitinib

Upadacitinib (ABT-494) 是高效选择性的，具有口服活性的 JAK1抑制剂，IC50为43 nM，可用于多种自身免疫性疾病的研究。它对 JAK1 的选择性约为 JAK2 的 74 倍。

CAS号

1310726-60-3

分子式

C17H19F3N6O

主要靶点

JAK

仅限科研使用

Cat No : CM04911

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Synonyms

ABT-494|乌帕替尼

验证数据展示

  • CAS No.: 1310726-60-3

    Upadacitinib
    CAS#: 1310726-60-3

产品信息

Upadacitinib (ABT-494) is a selective Janus kinase (JAK) 1 inhibitor, which is being studied for the treatment of several autoimmune disorders in the IC50 of 43 nM.

CAS号 1310726-60-3
分子式 C17H19F3N6O
主要靶点 JAK
主要通路 JAK/STAT信号通路|表观遗传|干细胞|血管生成
分子量 380.37
纯度 99.93%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 ABT-494|乌帕替尼

靶点活性

JAK1:43 nM|JAK2:200 nM

体内活性

Upadacitinib, a second JAK inhibitor, has been developed by AbbVie.Upadacitinib finished multiple-dose Phase I studies in 2013. Upadacitinib show to be safe and well-tolerated up to multiple doses of 24 mg twice daily using the immediate release formulation in phase I trials. Upadacitinib exposure is dose proportional to the evaluated multiple dose.

体外活性

Upadacitinib is 74-fold more selective for JAK-1 than for JAK-2, which is involved in erythropoiesis. And Upadacitinib is 58-fold more selective for JAK-1 than for JAK-3, which is involved in immunosurveillance. The enhanced selectivity of Upadacitinib for JAK-1 over JAK-2 and JAK-3 may offer an improved benefit-risk profile in patients with RA range.

溶解度

DMSO:22 mg/mL

参考文献

1.Nakayamada S, et al. Recent Progress in JAK Inhibitors for the Treatment of Rheumatoid Arthritis. BioDrugs. 2016 Oct;30(5):407-419.
2.Kremer JM, et al. A Phase IIb Study of ABT-494, a Selective JAK-1 Inhibitor, in Patients With Rheumatoid Arthritis and an Inadequate Response to Anti-Tumor Necrosis Factor Therapy. Arthritis Rheumatol. 2016Dec;68(12):2867-2877.

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