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).

[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.Harvard Medical School LINCS LIBRARY|BANGL J PHARMACOL. 2023 Dec 17.|Cancer Cell. 2018 Sep 10;34(3):439-452.e6. |Cancer Immunol Res. 2016 Jun;4(6):520-30.|Cancer Res. 2020 Jan 1;80(1):44-56. |Cell Death Dis. 2022 Dec 27;13(12):1075.|Cell Syst. 2018 Apr 25;6(4):424-443.e7.|Harvard Medical School LINCS LIBRARY|Immunol Invest. 2021 Oct 27;1-16.|Int J Biol Sci. 2022 Jan 1;18(2):585-598.|Int J Biol Sci. 2022; 18(2): 585-598.|J Pineal Res. 2019 Apr;66(3):e12552.|Leukemia. 2012 Oct;26(10):2233-44.|Sci Transl Med. 2018 Jul 18;10(450):eaaq1093.