Tofacitinib citrate

White to off-white powder. Soluble in DMSO (20mg/ml) or DMF (5 mg/ml). Slightly soluble in ethanol. Chemical. CAS: 540737-29-9. Formula: C16H20N6O . C6H8O7. MW: 312.4 . 192.1. Synthetic. Tofacitinib citrate is a potent cell permeable JAK3 inhibitor (IC50=1nM), which Shows also JAK-1 inhibitory activity. This is an immunosuppressive and anti-inflammatory agent. It inhibits signaling through heterodimeric receptors associated with JAK3, JAK1, or both of them, with functional selectivity over JAK2-paired receptors. Blocks downstream STAT signaling, resulting in potent inhibition of several cytokines, including interleukins 2, 4, 7, 9, 15 and 21, which are integral to lymphocyte activation, function and proliferation. It also has been shown to be a potent and selective inhibitor of HIV-1 replication and virus reactivation in vitro.