1. Epigenetics
    Stem Cell/Wnt
    JAK/STAT Signaling
  2. JAK
  3. Upadacitinib

Upadacitinib (Synonyms: ABT-494)

製品番号: HY-19569 純度: 99.96%
取扱説明書

Upadacitinib (ABT-494) is a potent, orally active and selective Janus kinase 1 (JAK1) inhibitor (IC50=43 nM). Upadacitinib (ABT-494) displays approximately 74 fold selective for JAK1 over JAK2 (200 nM) in cellular assays dependent on specific, relevant cytokines. Upadacitinib (ABT-494) is used in development for the treatment of several autoimmune disorders.

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Upadacitinib 構造式

Upadacitinib 構造式

CAS 番号 : 1310726-60-3

容量 価格(税別) 在庫状況 数量
無料サンプル (0.5-1 mg)   今すぐ申し込む  
10 mM * 1  mL in DMSO USD 50 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 110 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 160 在庫あり
Estimated Time of Arrival: December 31
25 mg USD 280 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 390 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 550 在庫あり
Estimated Time of Arrival: December 31
200 mg USD 850 在庫あり
Estimated Time of Arrival: December 31
500 mg USD 1500 在庫あり
Estimated Time of Arrival: December 31
1 g USD 2000 在庫あり
Estimated Time of Arrival: December 31
5 g USD 5000 在庫あり
Estimated Time of Arrival: December 31
10 g   お問い合わせ  
50 g   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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製品説明

Upadacitinib (ABT-494) is a potent, orally active and selective Janus kinase 1 (JAK1) inhibitor (IC50=43 nM). Upadacitinib (ABT-494) displays approximately 74 fold selective for JAK1 over JAK2 (200 nM) in cellular assays dependent on specific, relevant cytokines. Upadacitinib (ABT-494) is used in development for the treatment of several autoimmune disorders[1][2].

IC50 & Target[1]

JAK1

0.043 μM (IC50)

JAK2

0.2 μM (IC50)

JAK3

2.3 μM (IC50)

Tyk2

4.7 μM (IC50)

体外実験

In biochemical assays, Upadacitinib is 74-fold more selective for JAK-1 than for JAK-2 (which is involved in erythropoiesis) and 58-fold more selective for JAK-1 than for JAK-3 (which is involved in immunosurveillance)[1]. 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[2].

体内実験

Upadacitinib (0.1-10 mg/kg; oral gavage; twice a day for 10 days) demonstrates efficacy in rat arthritis models[3].

Animal Model: Female Lewis rats (Rat adjuvant-induced arthritis model)[3]
Dosage: 0.1, 0.3, 1, 3, 10 mg/kg
Administration: Oral gavage; twice a day for 10 days
Result: Inhibits disease pathology in rat adjuvant induced arthritis.
臨床実験
分子量

380.37

分子式

C₁₇H₁₉F₃N₆O

CAS 番号

1310726-60-3

SMILES

O=C(N1C[[email protected]@H](CC)[[email protected]@H](C2=CN=C3C=NC(NC=C4)=C4N32)C1)NCC(F)(F)F

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : ≥ 22 mg/mL (57.84 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6290 mL 13.1451 mL 26.2902 mL
5 mM 0.5258 mL 2.6290 mL 5.2580 mL
10 mM 0.2629 mL 1.3145 mL 2.6290 mL
*Please refer to the solubility information to select the appropriate solvent.
体内:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.67 mg/mL (4.39 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1.67 mg/mL (4.39 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 1.67 mg/mL (4.39 mM); Clear solution

*All of the co-solvents are provided by MCE.
参考文献

純度: 99.96%

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Keywords:

UpadacitinibABT-494ABT494ABT 494JAKJanus kinaseInhibitorinhibitorinhibit

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製品名:
Upadacitinib
製品番号:
HY-19569
数量:
MCE 日本正規代理店: