540737-29-9 Tofacitinib citrate AKSci X7518
 
 
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  X7518    AKSci Reference Standard
Tofacitinib citrate
, 98%
 



IDENTITY
CAS Number:540737-29-9
MDL Number:MFCD11616529
MF:C22H28N6O8
MW:504.49
SPECIFICATIONS & PROPERTIES
Min. Purity Spec:98%
Physical Form (at 20°C):Solid
Melting Point:214-218°C (subl.)
Long-Term Storage:Store long-term at -20°C
DOT/IATA TRANSPORT INFORMATION
Not hazardous material

BIOLOGICAL INFO
Solubility:DMSO
Application(s):JAK
Form:Citrate

REVIEW

 Tofacitinib (CP-690,550; CP-690550; CP690550), an orally active immunosuppressant, is being developed by Pfizer for the treatment of rheumatoid arthritis, inflammatory bowel disease, dry eyes, ankylosing spondylitis, psoriasis, psoriatic arthritis, and for the prevention of transplant rejection. Tofacitinib specifically inhibits Janus activated kinase 3 (JAK3), which has a pivotal role in cytokine signal transduction that governs lymphocyte survival, proliferation, differentiation, and apoptosis. It is currently approved for the treatment of rheumatoid arthritis (RA) in the United States and is being studied for treatment of psoriasis, inflammatory bowel disease, and other immunological diseases, as well as for the prevention of organ transplant rejection. Tofacitinib was not approved by the European regulatory agencies because of concerns over efficacy and safety.

REFERENCES
[1]Flanagan, Mark Edward; Li, Zheng Jane, Preparation of a novel crystalline compound useful as inhibitors of protein kinases PCT Int. Appl. (2003), WO 2003048162 A1 20030612.
[2] Mark E. Flanagan, Todd A. Blumenkopf, William H. Brissette, Matthew F. Brown, Jeffrey M. Casavant, Chang Shang-Poa, Jonathan L. Doty, Eileen A. Elliott, Michael B. Fisher, Michael Hines, Craig Kent, Elizabeth M. Kudlacz, Brett M. Lillie, Kelly S. Magnuson, Sandra P. McCurdy, Michael J. Munchhof, Bret D. Perry, Perry S. Sawyer, Timothy J. Strelevitz, Chakrapani Subramanyam, Jianmin Sun, David A. Whipple, and Paul S. Changelian, Disocovery of CP-690,550: A Potent and Selective Janus Kinase (JAK) Inhibitor for the Treatment of Autoimmune Diseases and Organ Transplant Rejection, Journal of Medicinal Chemistry (2010), 53(24), 8468-8484.
[3] Kremer JM, Bloom BJ, Breedveld FC, Coombs JH, Fletcher MP, Gruben D, Krishnaswami S, Burgos-Vargas R, Wilkinson B, Zerbini CA, Zwillich SH. The safety and efficacy of a JAK inhibitor in patients with active rheumatoid arthritis: Results of a double-blind, placebo-controlled phase IIa trial of three dosage levels of CP-690,550 versus placebo. Arthritis Rheum. 2009 Jul;60(7):1895-905. doi: 10.1002/art.24567.
[4] West K. CP-690550, a JAK3 inhibitor as an immunosuppressant for the treatment of rheumatoid arthritis, transplant rejection, psoriasis and other immune-mediated disorders. Curr Opin Investig Drugs. 2009 May;10(5):491-504.

GLOBALLY HARMONIZED SYSTEM (GHS)

Pictograms

Signal Word
Warning

Hazard Statements
H315; H319; H335

Precautionary Statements
P261; P264; P271; P280; P302+P352; P304+P340; P305+P351+P338; P312; P321; P332+P313; P337+P313; P362; P403+P233; P405; P501


Current as of June 22, 2024

AKSci Reference Standards are high-purity, low-impurity compounds suitable for use as standards.


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