Momelotinib (sulfate)

Momelotinib sulfate (CYT387 sulfate salt) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, 10-fold selectivity versus JAK3 (IC50=155 nM) .

Product Specifications

CAS Number

[1056636-06-6]

Product Name Alternative

CYT387 (sulfate salt)

UNSPSC

12352005

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-sulfate-salt.html

Purity

99.91

Solubility

DMSO : 220 mg/mL (ultrasonic) |H2O : 100 mg/mL (ultrasonic)

Smiles

O=C(NCC#N)C(C=C1)=CC=C1C2=NC(NC(C=C3)=CC=C3N4CCOCC4)=NC=C2.O=S(O)(O)=O.O=S(O)(O)=O

Molecular Formula

C23H26N6O10S2

Molecular Weight

610.62

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]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.|[3]Burns CJ, et al. Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs) . Bioorg Med Chem Lett. 2009 Oct 15;19 (20) :5887-92.