Momelotinib

Momelotinib (CYT387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50a of 11 nM and 18 nM, respectively. CYT387 shows much less activity against JAK3.

Product Specifications

CAS Number

[1056634-68-4]

Product Name Alternative

CYT387

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; Autophagy; JAK

Type

Reference compound

Related Pathways

Apoptosis; Autophagy; Epigenetics; JAK/STAT Signaling; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/CYT387.html

Concentration

10mM

Purity

99.37

Solubility

DMSO : 10 mg/mL (ultrasonic; warming; adjust pH to 3 with HCl; heat to 60°C)

Smiles

O=C(C1=CC=C(C2=NC(NC3=CC=C(N4CCOCC4)C=C3)=NC=C2)C=C1)NCC#N

Molecular Formula

C23H22N6O2

Molecular Weight

414.46

Precautions

H302, H315, H319, H335

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.|[4]Kitajima S, et al.Overcoming Resistance to Dual Innate Immune and MEK Inhibition Downstream of KRAS.Cancer Cell. 2018 Sep 10;34 (3) :439-452.e6.