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Ruxolitinib

Cat. No. 7064 3 Citations Submit a Review Datasheet / COA / SDS
Pricing Availability   Qty
Description: Potent and selective JAK1/JAK2 inhibitor; orally bioavailable
Alternative Names: INCB018424
Chemical Name: (3R)-3-Cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile
Purity: ≥98% (HPLC)
Datasheet
Citations (3)
Reviews
Pathways (1)
Biological Activity Technical Data Solubility Calculators Datasheets References

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

M. Wt 306.37
Formula C17H18N6
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 941678-49-5
PubChem ID 25126798
InChI Key HFNKQEVNSGCOJV-OAHLLOKOSA-N
Smiles N#CC[C@@H](N1C=C(C2=C3C=CNC3=NC=N2)C=N1)C4CCCC4

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
Solubility
DMSO 30.64 100

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.

Select a batch to recalculate based on the batch molecular weight:
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

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Product Datasheets for Ruxolitinib

Certificate of Analysis / Product Datasheet
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Safety Datasheet

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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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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Pathways for Ruxolitinib

JAK-STAT Signaling Pathway

JAK-STAT Signaling Pathway

The JAK-STAT signaling pathway has several roles, including the control of cell proliferation and hematopoiesis. It is the main signal transduction cascade from cytokine receptors.