Ruxolitinib

Biological Activity

Ruxolitinib is a potent and selective JAK1/2 inhibitor (IC₅₀ values are 3.3 and 2.8 nM, respectively). Exhibits selectivity for JAK1/2 over Tyk2 and JAK3 (~6-fold and >130-fold, respectively). Exhibits no significant inhibition against a commercial panel of 26 additional kinases. Inhibits JAK2V617F-mediated signaling and proliferation in Ba/F3 cells and HEL cells. Increases survival rates in a JAK2V617F-driven myeloproliferative neoplasm mouse model. Ruxolitinib has been identified as targeting human host proteins that interact with SARS-CoV-2. The compound can also be used in protocols for the chemical reprogramming of somatic cells to iPSCs. Orally bioavailable.

Phosphate salt (Cat. No. 7048) also available.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Enantioselective synthesis of Janus kinase inhibitor INCB018424 via an organocatalytic aza-Michael reaction.
   Lin et al.
   Org.Lett., 2009;11:1999
2. Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms.
   Quintás-Cardama et al.
   Blood, 2010;115:3109
3. A SARS-CoV-2-human protein-protein interaction map reveals drug targets and potential drug-repurposing.
   Gordon et al.
   Nature, 2020;

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