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

Upadacitinib (Synonyms: ABT-494)

Cat. No.: HY-19569 Purity: 99.40%
Data Sheet SDS Handling Instructions

Upadacitinib (ABT-494) is a potent and selective Janus kinase (JAK) 1 inhibitor being developed for the treatment of several autoimmune disorders with an IC50 of 43 nM.

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 $377 In-stock
1 mg $150 In-stock
5 mg $450 In-stock
10 mg $650 In-stock
25 mg $1350 Get quote
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  • Biological Activity

  • Protocol

  • Technical Information

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Description

Upadacitinib (ABT-494) is a potent and selective Janus kinase (JAK) 1 inhibitor being developed for the treatment of several autoimmune disorders with an IC50 of 43 nM.

IC50 & Target

IC50: 43 nM (JAK1), 200 nM (JAK2)[1]

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). 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

AbbVie’s second JAK inhibitor in development Upadacitinib has been described as a second-generation inhibitor. Multiple-dose Phase I studies are completed in 2013[1]. In phase I trials, Upadacitinib is found to be safe and well-tolerated up to multiple doses of 24 mg twice daily using the immediate release formulation. Upadacitinib exposure is dose proportional in the evaluated multiple dose[2].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT03006068 AbbVie Ulcerative Colitis (UC) January 31, 2017 Phase 3
NCT02782663 AbbVie Crohn's Disease (CD) May 18, 2016 Phase 2
NCT02706847 AbbVie Rheumatoid Arthritis March 15, 2016 Phase 3
NCT02955212 AbbVie Rheumatoid Arthritis October 15, 2017 Phase 3
NCT02819635 AbbVie Ulcerative Colitis (UC) September 28, 2016 Phase 2
NCT02925117 AbbVie Atopic Dermatitis January 30, 2017 Phase 2
NCT02720523 AbbVie Rheumatoid Arthritis March 22, 2016 Phase 2
NCT02629159 AbbVie Rheumatoid Arthritis March 9, 2014 Phase 3
NCT03086343 AbbVie Rheumatoid Arthritis May 9, 2017 Phase 3
NCT02706873 AbbVie Rheumatoid Arthritis February 23, 2016 Phase 3
NCT02675426 AbbVie Rheumatoid Arthritis December 17, 2015 Phase 3
NCT03104374 AbbVie Psoriatic Arthritis April 17, 2017 Phase 3
NCT02049138 AbbVie Rheumatoid Arthritis January 24, 2014 Phase 2
NCT02706951 AbbVie Rheumatoid Arthritis March 2, 2016 Phase 3
NCT02365649 AbbVie Crohn's Disease March 17, 2015 Phase 2
NCT02066389 AbbVie Rheumatoid Arthritis March 2014 Phase 2
NCT01741493 AbbVie (prior sponsor, Abbott)|AbbVie Rheumatoid Arthritis November 2012 Phase 1
NCT03104400 AbbVie Psoriatic Arthritis April 27, 2017 Phase 3
NCT01960855 AbbVie Rheumatoid Arthritis October 2013 Phase 2
NCT03006068 AbbVie Ulcerative Colitis (UC) January 31, 2017 Phase 3
NCT02782663 AbbVie Crohn's Disease (CD) May 18, 2016 Phase 2
NCT02706847 AbbVie Rheumatoid Arthritis March 15, 2016 Phase 3
NCT02955212 AbbVie Rheumatoid Arthritis October 15, 2017 Phase 3
NCT02819635 AbbVie Ulcerative Colitis (UC) September 28, 2016 Phase 2
NCT02925117 AbbVie Atopic Dermatitis January 30, 2017 Phase 2
NCT02720523 AbbVie Rheumatoid Arthritis March 22, 2016 Phase 2
NCT02629159 AbbVie Rheumatoid Arthritis March 9, 2014 Phase 3
NCT03086343 AbbVie Rheumatoid Arthritis May 9, 2017 Phase 3
NCT02706873 AbbVie Rheumatoid Arthritis February 23, 2016 Phase 3
NCT02675426 AbbVie Rheumatoid Arthritis December 17, 2015 Phase 3
NCT03104374 AbbVie Psoriatic Arthritis April 17, 2017 Phase 3
NCT02049138 AbbVie Rheumatoid Arthritis January 24, 2014 Phase 2
NCT02706951 AbbVie Rheumatoid Arthritis March 2, 2016 Phase 3
NCT02365649 AbbVie Crohn's Disease March 17, 2015 Phase 2
NCT02066389 AbbVie Rheumatoid Arthritis March 2014 Phase 2
NCT01741493 AbbVie (prior sponsor, Abbott)|AbbVie Rheumatoid Arthritis November 2012 Phase 1
NCT03104400 AbbVie Psoriatic Arthritis April 27, 2017 Phase 3
NCT01960855 AbbVie Rheumatoid Arthritis October 2013 Phase 2
NCT03178487 AbbVie Ankylosing Spondylitis August 6, 2017 Phase 2
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References
Molecular Weight

380.37

Formula

C₁₇H₁₉F₃N₆O

CAS No.

1310726-60-3

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 22 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Upadacitinib
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