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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 mouse model. Identified as targeting human host proteins that interact with SARS-CoV-2.Orally bioavailable.
Phosphate salt (Cat. No. 7048) also available.
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 306.37. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||3.26 mL||16.32 mL||32.64 mL|
|5 mM||0.65 mL||3.26 mL||6.53 mL|
|10 mM||0.33 mL||1.63 mL||3.26 mL|
|50 mM||0.07 mL||0.33 mL||0.65 mL|
References are publications that support the biological activity of the product.
Lin et al (2009) Enantioselective synthesis of Janus kinase inhibitor INCB018424 via an organocatalytic aza-Michael reaction. Org.Lett. 11 1999 PMID: 19385672
Quintás-Cardama et al (2010) Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms. Blood 115 3109 PMID: 20130243
Gordon et al (2020) A SARS-CoV-2-human protein-protein interaction map reveals drug targets and potential drug-repurposing. Nature 583 PMID: 32353859
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Keywords: Ruxolitinib, Ruxolitinib supplier, Potent, selective, JAK1/JAK2, inhibitors, inhibits, JAK1, JAK2, orally, bioavailable, active, in, vivo, COVID-19, SARS-CoV-2, severe, acute, respiratory, syndrome, INCB018424, JAK, Kinase, 7064, Tocris Bioscience
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