Tofacitinib Citrate

Name: Tofacitinib Citrate
SKU: T5720
Availability: InStock

Product ID T5720

Cas No. 540737-29-9

Purity ≥99%

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Product Info
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Description

Tofacitinib is an inhibitor of JAK1/2/3 that is clinically used to treat myelofibrosis and rheumatoid arthritis. Tofacitinib exhibits immunosuppressive, anti-inflammatory, and antiviral activities. In vitro, tofacitinib inhibits production of inflammatory cytokines, Th2 cell differentiation, Th17 cell differentiation, and activation of STAT1, which in turn prevents induction of T-bet and generation of Th1 cells. In other cellular models, tofacitinib inhibits HIV replication and reactivation of latent HIV-1.

Product Info

Cas No.	540737-29-9
Purity	≥99%
Formula	C₁₆H₂₀N₆O • C₆H₈O₇
Formula Wt.	504.49
Chemical Name	3-[(3R,4R)-4-methyl-3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]-3-oxopropanenitrile citrate salt
IUPAC Name	2-hydroxypropane-1,2,3-tricarboxylic acid;3-[(3R,4R)-4-methyl-3-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]-3-oxopropanenitrile
Synonym	CP-690550-10, Tasocitinib citrate salt
Solubility	Soluble in DMSO (100 mg/ml at 25 °C), ethanol (<1 mg/ml at 25 °C), DMF (~5 mg/ml), water (<1 mg/ml at 25 °C), and 0.5% methylcellulose (30 mg/ml at 25 °C)
Appearance	White to off white powder

Shipping and Storage

Store Temp	Ambient
Ship Temp	Ambient

Downloads

MSDS	T5720 MSDS PDF
Info Sheet	T5720 Info Sheet PDF

References

Gavegnano C, Detorio M, Montero C, et al. Ruxolitinib and Tofacitinib are Potent and Selective Inhibitors of HIV-1 Replication and Virus Reactivation in Vitro. Antimicrob Agents Chemother. 2014 Jan 13. [Epub ahead of print]. PMID: 24419350.

Yamaoka K, Tanaka Y. Targeting the Janus kinases in rheumatoid arthritis: focus on tofacitinib. Expert Opin Pharmacother. 2014 Jan;15(1):103-13. PMID: 4188100.

Tak PP, Kalden JR. Advances in rheumatology: new targeted therapeutics. Arthritis Res Ther. 2011 May 25;13 Suppl 1:S5. PMID: 21624184.

Ghoreschi K, Jesson MI, Li X, et al. Modulation of innate and adaptive immune responses by tofacitinib (CP-690,550). J Immunol. 2011 Apr 1;186(7):4234-43. PMID: 21383241.