Momelotinib (mesylate)
Momelotinib mesylate (CYT387 mesylate) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, appr 10-fold selectivity versus JAK3.
Product Specifications
CAS Number
[1056636-07-7]
Product Name Alternative
CYT387 (mesylate)
UNSPSC
12352005
Target
Autophagy; JAK
Type
Reference compound
Related Pathways
Autophagy; Epigenetics; JAK/STAT Signaling; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt
Applications
COVID-19-immunoregulation
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/CYT387-Mesylate.html
Solubility
10 mM in DMSO
Smiles
O=C(C1=CC=C(C2=NC(NC3=CC=C(N4CCOCC4)C=C3)=NC=C2)C=C1)NCC#N.O=S(O)(C)=O
Molecular Formula
C24H26N6O5S
Molecular Weight
510.57
References & Citations
[1]Pardanani A, et al. CYT387, a selective JAK1/JAK2 inhibitor: in vitro assessment of kinase selectivity and preclinical studies using cell lines and primary cells from polycythemia vera patients. Leukemia, 2009, 23 (8), 1441-1445.|[2]Monaghan KA, et al. The novel JAK inhibitor CYT387 suppresses multiple signalling pathways, prevents proliferation and induces apoptosis in phenotypically diverse myeloma cells. Leukemia, 2011, 25 (12), 1891-1899.|[3]Tyner JW, et al. CYT387, a novel JAK2 inhibitor, induces hematologic responses and normalizes inflammatory cytokines in murine myeloproliferative neoplasms. Blood, 2010, 115 (25), 5232-5240.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
Phase 3
Isoform
JAK1; JAK2; JAK3
Curated Selection
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