Cyt387 CAS NO.1056634-68-4

cyt387(momelotinib) is an atp-competitive inhibitor of jak1/jak2 with ic50 of 11 nm/18 nm, ~10-fold selectivity versus jak3.
ic50 value: 11 nm/18 nm(jak1/jak2) [1]
target: jak1/jak2
in vitro: cyt387 inhibits the proliferation of parental ba/f3 cells (ba/f3-wt) stimulated by il-3 with ic50 of 1400 nm. furthermore, cyt387 also causes the inhibition of cell proliferation in cell lines constitutively activated by jak2 or mpl signaling, including ba/f3-mplw515l cells, chrf-288-11 cells and ba/f3-tel-jak2 cells with ic50 of 200 nm, 1 nm and 700 nm, respectively. in addition, cyt387 has been shown to inhibit erythroid colony growth in vitro from jak2v617f-positive pv patients with similar potency with ic50 of 2μ-4 μm [1]. a recent study shows that cyt387 inhibits pi3k/akt and ras/mapk signaling induced by il-6 and igf-1. moreover, cyt387 induces apoptosis as a single agent and synergizes with the conventional anti-mm therapies bortezomib and melphalan in primary multiple myeloma (mm) cells [2].
in vivo: in a murine mpn model, cyt387 normalizes white cell counts, hematocrit, spleen size, and restores physiologic levels of inflammatory cytokines [3].