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Biological Activity for Ruxolitinib
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.
Compound Libraries for Ruxolitinib
Ruxolitinib is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library, Tocriscreen Antiviral Library, Tocriscreen Epigenetics Library and Tocriscreen FDA-Approved Drugs. Find out more about compound libraries available from Tocris.
Technical Data for Ruxolitinib
|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.
Solubility Data for Ruxolitinib
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for Ruxolitinib
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 for Ruxolitinib
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
Guan et al (2022) Chemical reprogramming of human somatic cells to pluripotent stem cells Nature 605 325 PMID: 35418683
If you know of a relevant reference for Ruxolitinib, please let us know.
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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, induced, pluripotent, stem, cells, reprogramming, iPSC, INCB018424, JAK, Kinase, Coronavirus, Stem, Cell, Reprogramming, 7064, Tocris Bioscience
3 Citations for Ruxolitinib
Citations are publications that use Tocris products. Selected citations for Ruxolitinib include:
Chin Wai et al (2022) Interleukins 4 and 21 Protect Anti-IgM Induced Cell Death in Ramos B Cells: Implication for Autoimmune Diseases. Front Immunol 13 919854 PMID: 35911775
Anastasia et al (2022) RNAi-based modulation of IFN-γ signaling in skin. Mol Ther 30 2709-2721 PMID: 35477658
Jung Mo et al (2023) Endothelial cell-derived stem cell factor promotes lipid accumulation through c-Kit-mediated increase of lipogenic enzymes in brown adipocytes. Nat Commun 14 2754 PMID: 37179330
Do you know of a great paper that uses Ruxolitinib from Tocris? Please let us know.
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Literature in this Area
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