tcsc0326 Ruxolitinib (phosphate)

Ruxolitinib (phosphate) is the first potent JAK1/2 inhibitor with IC₅₀ values of 3.3 nM/2.8 nM, more than 130-fold selectivity for JAK1/2 versus JAK3.

IC50 & Target: IC50: 3.3 nM (JAK1), 2.8 nM (JAK2)

In Vitro: Ruxolitinib (INCB018424) potently and selectively inhibits JAK2V617F-mediated signaling and proliferation. Ruxolitinib inhibits the growth of HEL cells with EC₅₀ of 186 nM. Ruxolitinib markedly increases apoptosis in Ba/F3-EpoR-JAK2V617F cell system, and inhibits hematopoietic progenitor cell proliferation in primary MPN patient samples^[1].

In Vivo: Ruxolitinib (180 mg/kg, p.o.) reduces the tumor burden of mice inoculated with JAK2V617F-expressing cells without causing anemia or lymphopenia^[1].