905586-69-8

Solubility:Soluble in DMSO at 10 mM,

Biologieal

CP690550(Tasocitinib),the only Janus Kinase 3 (JAK3) inhibitor currently in clinical trials,an immunosuppressive agent exhibiting potent effects in preclinical transplantation and arthritis models; clinically safe and effective in preventing transplant rejection and improving symptoms of rheumatoid arthritis and psoriasis. CP690550(Tasocitinib) treatment of murine factor-dependent cell Patersen-erythropoietin receptor (FDCP-EpoR) cells harboring human wild-type or V617F JAK2 resulted in inhibition of cell proliferation with a IC50 of 2.1µM and 0.25 µM, respectively. Furthermore, CP690550(Tasocitinib) treatment of ex-vivo-expanded erythroid progenitors from JAK2(V617F)-positive PV patients resulted in specific, antiproliferative (IC50 = 0.2µM) and pro-apoptotic activity. In contrast, expanded progenitors from healthy controls were less sensitive to CP690550 in proliferation (IC50 > 1.0 µM), and apoptosis assays.

Reference

1. AC Papageorgiou and LEK Wikman, Is JAK3 a new drug target for immunomodulation-based therapies? Trends Pharmacol. Sci. 2004, 25(11), 558-562.SOLUB

2. E. Kudlacz, et al. The JAK-3 inhibitor CP690550 is a potent anti-inflammatory agent in a murine model of pulmonary eosinophilia. Eur J Pharmacol. 2008, 582(1-3), 154-61. 3. PS Changelian et al. Prevention of Organ Allograft Rejection by a Specific Janus Kinase