Ruxolitinib

JAK1 & JAK2 Inhibitor

Ruxolitinib (INCB018424) is a small-molecule ATP mimetic. It is an inhibitor of both JAK1 and JAK2, results in a dramatic decrease in levels of inflammatory cytokines, IL-6 and TNF-α [1].

Ruxolitinib is clinically used for the treatment of myelofibrosis, a bone marrow disorder [2], and is being investigated for the treatment of certain cancers and autoimmune diseases, such as psoriasis.

References:

1. Quintás-Cardama A., 2010. Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms. Blood 115(15):3109-17.
2. Mascarenhas J. & Hoffman R., 2012. Ruxolitinib: The first FDA approved therapy for the treatment of myelofibrosis. Clin Cancer Res. 18:3008-14.

Figures

Effect of Ruxolitinib on HEK-Blue™ IFN-α/β cell response to type I and type III IFNs: HEK‑Blue™ IFN-α/β cells were incubated with 3 U/ml hIFN-α2b (grey), 1 U/ml hIFN-β1 (purple) or 10 ng/ml hIL-29 (hIFN-λ1) (red) and increasing concentrations of Ruxolitinib. After 24h incubation, IFN-induced ISG activation was assessed by measuring SEAP levels in the supernatant using QUANTI‑Blue™. Percentages of maximal response (no inhibitor) for each cytokine are shown.

Specifications

Synonym: Ruxolitinib phosphate, INCB018424

CAS number: 1092939-17-7

Formula: C₁₇H₁₈N₆, H₃O₄P

Molecular weight: 404.36

Solubility: 10 mg/ml in DMSO

Quality control:

• Purity ≥97% (UHPLC)
• The absence of bacterial contamination (e.g. lipoproteins and endotoxins) is confirmed using HEK-Blue™ TLR2 and HEK-Blue™ TLR4 cells.

Contents

Ruxolitinib is provided as a translucent film

• 5 mg Ruxolitinib

Ruxolitinib is  shipped at room temperature.

Store at -20 °C.

Solid product is stable 2 years when properly stored.