Upadacitinib (tartrate tetrahydrate)

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

Product Specifications

CAS Number

[1607431-21-9]

Product Name Alternative

ABT-494 (tartrate tetrahydrate)

UNSPSC

12352005

Hazard Statement

H302-H312-H332

Target

JAK

Related Pathways

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

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Solubility

10 mM in DMSO

Smiles

O=C(NCC(F)(F)F)N1C[C@H]([C@H](C1)C2=CN=C3C=NC4=C(N32)C=CN4)CC.O=C([C@@H]([C@H](C(O)=O)O)O)O.[4.H2O]

Molecular Formula

C17H19F3N6O.C4H6O6.4H2O

Molecular Weight

602.52

Precautions

P261-P264-P270-P271-P280-P302+P352-P304+P340-P330-P363-P501

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.