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Upadacitinib

Catalog No. T7503 CAS 1310726-60-3

Synonyms: ABT-494

Upadacitinib (ABT-494) (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.

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Upadacitinib, CAS 1310726-60-3

Pack Size	Availability	Price/USD
1 mg	In stock	$ 39.00
2 mg	In stock	$ 56.00
5 mg	In stock	$ 91.00
10 mg	In stock	$ 132.00
25 mg	In stock	$ 232.00
50 mg	In stock	$ 323.00
100 mg	In stock	$ 457.00
200 mg	In stock	$ 697.00
500 mg	In stock	$ 1,230.00
1 mL * 10 mM (in DMSO)	In stock	$ 41.00

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Purity: 99.93%

Purity: 99.89%

Purity: 99.78%

Purity: 99.41%

Biological Description

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Storage & Solubility Information

Description	Upadacitinib (ABT-494) (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.
Targets&IC50	JAK2:200 nM, JAK1:43 nM
In vitro	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.
In vivo	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.

Synonyms	ABT-494
Molecular Weight	380.37
Formula	C17H19F3N6O
CAS No.	1310726-60-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 22 mg/mL

References and Literature

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.

Citations

1. Si H, Wang J, He R, et al. Identification of U937JAK3-M511I Acute Myeloid Leukemia Cells as a Sensitive Model to JAK3 Inhibitor. Frontiers in oncology. 2021, 11: 807200-807200. 2. Wang F, Wang S, Zhang C, et al.Noncanonical JAK1/STAT3 interactions with TGF-β modulate myofibroblast transdifferentiation and fibrosis.American Journal of Physiology-Lung Cellular and Molecular Physiology.2022, 323(6): L698-L714.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Inhibitor Library Highly Selective Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Drug Library Anti-Cancer Approved Drug Library EMA Approved Drug Library Anti-Lung Cancer Compound Library Pediatric Drug Library Human Metabolite Library

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Keywords

Upadacitinib 1310726-60-3 Angiogenesis Chromatin/Epigenetic JAK/STAT signaling Stem Cells JAK ABT 494 inhibit Inhibitor autoimmune orally active JAK1 ABT-494 Janus kinase ABT494 inhibitor

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