A JAK1 inhibitor (IC50 = 47 nM); selective for JAK1 over JAK3 and Tyk2 (IC50s = 2

Upadacitinib – 10 mg

Brand:
Cayman
CAS:
1310726-60-3
Storage:
-20
UN-No:
Non-Hazardous - /

Upadacitinib is a JAK1 inhibitor (IC50 = 47 nM).{49501} It is selective for JAK1 over JAK3 and tyrosine kinase 2 (Tyk2; IC50s = 2,304 and 4,690 nM, respectively), as well as a panel of 83 additional kinases at 1 µM, but does inhibit JAK2, Rho-associated kinase I (ROCK-I), and ROCK-II (IC50s = 120, 920, and 430 nM, respectively). Upadacitinib decreases cytokine-induced STAT phosphorylation in a variety of human cells with IC50 values ranging from 1.6 to 649 nM. It reduces M. tuberculosis-induced paw swelling and bone erosion in a rat model of arthritis when administered at doses of 1, 3, and 10 mg/kg twice per day for 17 days. Formulations containing upadacitinib have been used in the treatment of rheumatoid arthritis.  

 

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Description

A JAK1 inhibitor (IC50 = 47 nM); selective for JAK1 over JAK3 and Tyk2 (IC50s = 2,304 and 4,690 nM, respectively), as well as a panel of 83 additional kinases at 1 µM, but does inhibit JAK2, ROCK-I, and ROCK-II (IC50s = 120, 920 and 430 nM, respectively); decreases cytokine-induced STAT phosphorylation in a variety of human cells (IC50s = 1.6-649 nM); reduces M. tuberculosis-induced paw swelling and bone erosion in a rat model of arthritis at 1, 3, and 10 mg/kg twice per day for 17 days

Formal name: (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)-1-pyrrolidinecarboxamide

Synonyms:  ABT-494

Molecular weight: 380.4

CAS: 1310726-60-3

Purity: ≥98%

Formulation: A crystalline solid

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