Upadacitinib tartrate

Product NameUpadacitinib tartrate
CAS1607431-21-9
MFC21H25F3N6O7
MW530.46
EINECS
MOL File1607431-21-9.mol

Usage And Synthesis

Uses

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].

in vivo

Upadacitinib (0.1-10 mg/kg; oral gavage; twice a day for 10 days) tartrate tetrahydrate 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:	Inhibited disease pathology in rat adjuvant induced arthritis.

IC 50

JAK1: 0.043 μM (IC₅₀); JAK2: 0.2 μM (IC₅₀); JAK3: 2.3 μM (IC₅₀); Tyk2: 4.7 μM (IC₅₀)

References

[1] Nakayamada S, et al. Recent Progress in JAK Inhibitors for the Treatment of Rheumatoid Arthritis. BioDrugs. 2016 Oct;30(5):407-419. DOI:10.1007/s40259-016-0190-5
[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. DOI:10.1186/s41927-018-0031-x