Ruxolitinib

Name: Ruxolitinib
Brand: Tocris Bioscience
SKU: 7064

Tocris Bioscience, part of Bio-Techne | Catalog # 7064

Citations (16)

COA / SDS

Potent and selective JAK1/JAK2 inhibitor; orally bioavailable

Key Product Details

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)
Molecular Weight:	306.37

View Full Technical Details for Ruxolitinib

Technical Data
Citations

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 for Ruxolitinib

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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.

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 for Ruxolitinib

References are publications that support the biological activity of the product.

Guan Chemical reprogramming of human somatic cells to pluripotent stem cells Nature 2022 PMID: 35418683
Quintás-Cardama Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms. Blood 2010 PMID: 20130243
Gordon A SARS-CoV-2-human protein-protein interaction map reveals drug targets and potential drug-repurposing. Nature 2020 PMID: 32353859
Lin Enantioselective synthesis of Janus kinase inhibitor INCB018424 via an organocatalytic aza-Michael reaction. Org.Lett. 2009 PMID: 19385672