Momelotinib

  • Chemical Properties
CAS No. 1056634-68-4 Cat. No. BCP02328
Name Momelotinib
Synonyms CYT 11387;CYT-387;CYT387;
Formula C23H22N6O2 M. Wt 414.46
  • Biological Activity
Description 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.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.
Pathways Angiogenesis/Protein Tyrosine Kinase Jak/Stat Pathway Wnt/Stem Cell Epigenetics 
Targets JAK 

Structure

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