Tofacitinib (CP-690550) is a potent, specific, orally active inhibitor of JAK3 with IC50 of 1 nM in cell-free assays.
Tofacitinib (CP-690550) displays 20- to 100-fold less potency for JAK2 and JAK1 (IC50=20 nM and 112 nM, respectively), and shows no potent activity against 30 other kinases at >3 uM (CaMK1, ROCK2, Lck, MST2, etc.).
Tofacitinib (CP-690550) effectively inhibits a murine mixed lymphocyte reaction (MLR) with IC50 of 91 nM.
Tofacitinib (CP-690550) significantly prolonges survival in a murine model of heart transplantation and in cynomolgus monkeys receiving kidney transplants.
Physicochemical Properties
M.Wt
312.37
Formula
C16H20N6O
Appearance
Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility
DMSO: 100 mM (31.2 mg/mL); H2O: <1 mM (<0.3 mg/mL)
