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

Upadacitinib (Synonyms: ABT-494)

Cat. No.: HY-19569 Purity: 99.96%
Handling Instructions

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.

For research use only. We do not sell to patients.

Upadacitinib Chemical Structure

Upadacitinib Chemical Structure

CAS No. : 1310726-60-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 50 In-stock
Estimated Time of Arrival: December 31
5 mg USD 110 In-stock
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10 mg USD 160 In-stock
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25 mg USD 280 In-stock
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50 mg USD 390 In-stock
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100 mg USD 550 In-stock
Estimated Time of Arrival: December 31
200 mg USD 850 In-stock
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500 mg USD 1500 In-stock
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1 g USD 2000 In-stock
Estimated Time of Arrival: December 31
5 g USD 5000 Get quote
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Based on 1 publication(s) in Google Scholar

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Description

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)

In Vitro

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].

In Vivo

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.
Clinical Trial
Molecular Weight

380.37

Formula

C₁₇H₁₉F₃N₆O

CAS No.

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

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.
In Vivo:
  • 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.
References

Purity: 99.96%

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Keywords:

UpadacitinibABT-494ABT494ABT 494JAKJanus kinaseInhibitorinhibitorinhibit

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Product name:
Upadacitinib
Cat. No.:
HY-19569
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