Ruxolitinib

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Cat.No. 7064 - Ruxolitinib | C17H18N6 | CAS No. 941678-49-5
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
Reviews
Literature (3)
Pathways (1)

Biological Activity

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.

Technical Data

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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 30.64 100
ethanol 6.13 20

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.

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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References

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 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

Citations for Ruxolitinib

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!

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Cancer

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Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

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Pathways for Ruxolitinib

JAK-STAT

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.