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.