InformationUpadacitinib (ABT-494) is a selectiveJAK1inhibitor which demonstrates activity against JAK1 (0.045 μM) and JAK2 (0.109 μM), with > 40 fold selectivity over JAK3 (2.1 μM) and 100 fold selectivity over TYK2 (4.7 μM) as compared to JAK1.In vitroUpadacitinib is most potent on JAK1compared to other family members (JAK1/u2009>/u2009JAK2/u2009>/u2009JAK3/u2009>/u2009TYK2). Upadacitinib demonstrates selectivity across a broad panel of 70+ kinases, with only Rock1 and Rock2 demonstrating IC50 values below 1 μM. Consistent with the Ba/F3 cellular data, upadacitinib potently inhibits the JAK1 dependent cytokines IL-6, OSM, IL-2, and IFNγ, as measured by inhibition of STAT phosphorylation.In vivoUpadacitinib inhibits disease pathology in rat adjuvant induced arthritis. It is a non-sensitive substrate for cytochrome P450, approximately 20% is eliminated, unchanged, in urine.Cell Datacell lines：Concentrations：Incubation Time：Powder Purity:≥99%. Specification: 10mM in DMSO Molecular Formula: C17H19F3N6O Molecular Weight: 380.37
- UPC:
- 51202000
- Condition:
- New
- Availability:
- 2 weeks
- Weight:
- 0.85 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- U408740-1ml
- CAS:
- 1310726-60-3
- Product Size:
- 1ml
