Upadacitinib

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) can be used for several autoimmune disorders research[1][2].

Product Specifications

CAS Number

[1310726-60-3]

Product Name Alternative

ABT-494

UNSPSC

12352005

Hazard Statement

H315, H319, H335

Target

JAK

Type

Reference compound

Related Pathways

Epigenetics; JAK/STAT Signaling; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/Upadacitinib.html

Purity

99.98

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C17H19F3N6O

Molecular Weight

380.37

Precautions

H315, H319, H335

References & Citations

[1]Nakayamada S, et al. Recent Progress in JAK Inhibitors for the Treatment of Rheumatoid Arthritis. BioDrugs. 2016 Oct;30 (5) :407-419.|[2]J. Voss, et al. THU0127 Pharmacodynamics of A Novel JAK1 Selective Inhibitor in Rat Arthritis and Anemia Models and in Healthy Human Subjects. doi 10.1136/annrheumdis-2014-eular.3823.|[3]Parmentier JM, et al. In vitro and in vivo characterization of the JAK1 selectivity of upadacitinib (ABT-494) . BMC Rheumatol. 2018 Aug 28;2:23.