CP 690550 citrate

Cat. No. 4556

CP 690550 citrate C16H20N6O.C6H8O7 [540737-29-9]

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Alternative Name: Tofacitinib citrate

Chemical Name: (3R,4R)-4-Methyl-3-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-β-oxo-1-piperidinepropanenitrile citrate

Biological Activity

Potent JAK inhibitor (IC50 values are 1, 20, and 112 nM for JAK3, JAK2 and JAK1 respectively). Orally active immunosuppressant; exhibits efficacy in rodent rheumatoid arthritis models.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

External Portal Information

Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of CP 690550 (Tofacitinib) is reviewed on the chemical probes website.

Technical Data

M.Wt:
504.49
Formula:
C16H20N6O.C6H8O7
Solubility:
Soluble to 100 mM in DMSO
Purity:
>99 %
Storage:
Store at +4°C
CAS No:
540737-29-9

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

Dowty et al (2013) Preclinical to clinical translation of tofacitinib, a Janus kinase inhibitor, in rheumatoid arthritis. J.Pharmacol.Exp.Ther. 348 165. PMID: 24218541.

Flanagan et al (2010) Discovery of CP-690,550: a potent and selective Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases and organ transplant rejection. J.Med.Chem. 53 8468. PMID: 21105711.

Jiang et al (2008) Examining the chirality, conformation and selective kinase inhibition of 3-((3R,4R)-4-methyl-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)-3-oxopropanenitrile (CP-690,550). J.Med.Chem. 51 8012. PMID: 19053756.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for CP 690550 citrate include:

Tactacan et al (2015) The pseudokinase SgK223 promotes invasion of pancreatic ductal epithelial cells through JAK1/Stat3 signaling. Mol Cancer 14 139. PMID: 26215634.

Zhu et al (2015) Adenosine 5'-monophosphate-activated protein kinase regulates IL-10-mediated anti-inflammatory signaling pathways in macrophages. Nat Commun 194 584. PMID: 25512602.

Do you know of a great paper that uses CP 690550 citrate from Tocris? If so please let us know.

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Keywords: CP 690550 citrate, supplier, CP690550, immunosuppressants, autoimmune, antirheumatics, rheumatoid, arthritis, pfizer, JAK, janus, kinase, JAK1, JAK2, JAK3, inhibitors, inhibits, Tofacitinib, Tocris Bioscience, JAK Kinase Inhibitor products

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