Biological Activity
Tofacitinib citrate is provided as the citrate salt form of Tofacitinib free base. It is the active ingredient of the drug sold under the trade name Xeljanz® for the treatment of rheumatoid arthritis (RA) in at least one country. It is currently undergoing clinical trials for psoriasis, inflammatory bowel disease, and other immune mediated diseases. [Note: Tofacitinib citrate sold by Gene Operation is for scientific research use only, not for human and veterinary use.]
Tofacitinib (CP-690550) is a potent, selective, and ATP-competitive JAK inhibitor, suppressing all four JAK isoforms with nM potency in vitro enzyme assays (IC50 values are 3.2 nM, 4.1 nM, 1.6 nM, and 34 nM for JAK1, JAK2, JAK3, and TYK2, respectively), but significantly inhibiting signaling through JAK1 and JAK3 with 5-100 fold selectivity over JAK2 in cellular assays. This agent is being developed as an immunosuppressive and anti-inflammatory drug for the treatment and prevention of acute allograft rejection, RA, psoriasis and other immune mediated diseases [1]. CP-690550 shows great efficacy in various rodent and nonhuman primate models of allograft organ transplantation [2-4], as well as rodent models of RA [1, 5].
Chemical Properties
Cas No.: 540737-29-9 |
M. Wt.: 504.49 |
Formula: C16H20N6O•C6H8O7 |
Purity: >99% |
Synonym: CP-690550 Citrate, Tasocitinib Citrate, Xeljanz® |
Chemical Name: (3R,4R)-4-Methyl-3-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-β-oxo-1-piperidinepropanenitrile citrate |
Appearance: White to off-white solid |
Solubility: Soluble in DMSO up to 100 mM |
Storage:Store solid at -20 ºC for the stability of two years |
Application Concentration (Just for reference)
The appropriate working concentration of Tofacitinib citrate depends on cell types, cell culture properties and specific applications. It is recommended that researchers start with optimal experiments for first use.