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PZ0017 Sigma-Aldrich

Tofacitinib citrate

≥98% (HPLC)

Synonym: (3R,4R)-4-Methyl-3-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-β-oxo-1-piperidinepropanenitrile citrate salt, 3-[(3R,4R)-4-Methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]-3-oxopropanenitrile citrate salt, CP-690550-10, Tasocitinib citrate salt

  • CAS Number 540737-29-9

  • Empirical Formula (Hill Notation) C16H20N6O · C6H8O7

  • Molecular Weight 504.49

  •  MDL number MFCD11616529

  •  PubChem Substance ID 329823686

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Properties

Related Categories Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Cell Biology, Cell Signaling and Neuroscience, Janus Kinase (JAK),
InChI Key   SYIKUFDOYJFGBQ-YLAFAASESA-N
assay   ≥98% (HPLC)
form   powder
color   white to beige
solubility   DMSO: 5 mg/mL (clear solution; warmed)
originator   Pfizer
storage temp.   room temp

Description

Other Notes

This compound was developed by Pfizer for Kinase Phosphatase Biology research. To learn more about Sigma′s partnership with Pfizer and view other authentic, high-quality Pfizer compounds, visit sigma.com/bsm-pfizer.

To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Tofacitinib has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the Tofacitinib probe summary on the Chemical Probes Portal website.

Packaging

5, 25 mg in glass bottle

Legal Information

Sold for research purposes under agreement from Pfizer Inc.

Application

Tofacitinib citrate has been used:
• as a ligand for human serum albumin in fluorescence quenching, dynamic light scattering (DLS) measurements, differential scanning calorimetry and molecular docking studies
• as a medium supplement for full depth articular cartilage (FDC) explants to monitor cytokine-induced proteoglycan loss
• as a Janus kinase inhibitor in MCF7 breast cancer cells

Biochem/physiol Actions

Tofacitinib is a potent inhibitor of Janus kinase 3 (JAK3) with some JAK-1 inhibitory activity as well. It blocks downstream STAT signaling resulting in potent inhibition of inflammatory cytokines with resultant immunosuppressive and anti-inflammatory activity. Tofacitinib is being investigated for for several autoimmune disorders including, rheumatoid arthritis, psoriasis and dry eye.

Features and Benefits

This compound is a featured product for Kinase Phosphatase Biology research. Click here to discover more featured Kinase Phosphatase Biology products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

General description

Tofacitinib is a synthetic molecule corresponding to a molecular weight of 312.4 Da and is permeable by transcellular diffusion.

Safety & Documentation

Safety Information

RIDADR 
NONH for all modes of transport
WGK Germany 
3

Documents

Certificate of Analysis


Milli-Q® Water Purification Solutions
Protocols & Articles

Articles

Discover Bioactive Small Molecules for Kinase Phosphatase Biology

Phosphorylation is a ubiquitous cellular regulatory mechanism that mediates signal transduction pathways, which carry signals from the cell surface to the nucleus or cytoplasm, by altering the activi...
Keywords: Apoptosis, Bioactive small molecules, Cancer, Diseases, Inflammation, Metabolism, Neurodegenerative Diseases, Phosphorylations, Transduction

Pfizer Compounds for Kinase Phosphatase Biology

From our library of Articles, Sigma-Aldrich presents Pfizer Compounds for Kinase Phosphatase Biology

Peer-Reviewed Papers
15

References

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