Momelotinib (CYT387)

InformationMomelotinib (CYT387, LM-1149 , CYT11387) is an ATP-competitive inhibitor ofJAK1/JAK2withIC50of 11 nM/18 nM, ~10-fold selectivity versus JAK3. Momelotinib (CYT387) inducesapoptosisandautophagy. Phase 3.In vitroCYT387 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. 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.In vivoIn a murine MPN model, CYT387 normalizes white cell counts, hematocrit, spleen size, and restores physiologic levels of inflammatory cytokines.Cell Datacell lines：Concentrations：0 to 10 μMIncubation Time：72 hoursPowder Purity:≥95%. Specification: 10mM in DMSO Molecular Formula: C23H22N6O2 Molecular Weight: 414.46