CP 690550 citrate

Pricing Availability   Qty
Description: Potent JAK inhibitor
Alternative Names: Tofacitinib citrate
Chemical Name: (3R,4R)-4-Methyl-3-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-β-oxo-1-piperidinepropanenitrile citrate
Purity: ≥99% (HPLC)
Citations (6)
Reviews (1)
Pathways (1)

Biological Activity for CP 690550 citrate

CP 690550 citrate is a 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 for CP 690550 citrate

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.

Compound Libraries for CP 690550 citrate

CP 690550 citrate 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 CP 690550 citrate

M. Wt 504.49
Formula C16H20N6O.C6H8O7
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 540737-29-9
PubChem ID 10174505
Smiles C[C@H]1[C@@H](N(C2=NC=NC3=C2C=CN3)C)CN(C(CC#N)=O)CC1.OC(CC(O)=O)(C(O)=O)CC(O)=O

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 CP 690550 citrate

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 50.45 100

Preparing Stock Solutions for CP 690550 citrate

The following data is based on the product molecular weight 504.49. 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 1.98 mL 9.91 mL 19.82 mL
5 mM 0.4 mL 1.98 mL 3.96 mL
10 mM 0.2 mL 0.99 mL 1.98 mL
50 mM 0.04 mL 0.2 mL 0.4 mL

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Product Datasheets for CP 690550 citrate

References for CP 690550 citrate

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

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

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

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

If you know of a relevant reference for CP 690550 citrate, please let us know.

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6 Citations for CP 690550 citrate

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

Tetsuro et al (2020) Targeted therapy guided by single-cell transcriptomic analysis in drug-induced hypersensitivity syndrome: a case report. Nat Med 26 236-243 PMID: 31959990

Eun-Kyoung et al (2017) The Peptidylarginine Deiminase Inhibitor Cl-Amidine Suppresses Inducible Nitric Oxide Synthase Expression in Dendritic Cells. Int J Mol Sci 18 PMID: 29077055

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

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

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

Reviews for CP 690550 citrate

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Worked for cytokine Elisa analysis.
By Scott Scarneo on 02/06/2019
Assay Type: Ex Vivo
Species: Human
Cell Line/Tissue: RA FLS

Used for RA FLS Cytokine production of IL-6.

review image

Pathways for CP 690550 citrate

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.