|
Biological Activity:
Selective and ATP-competitive Janus Kinase JAK1/JAK2 inhibitor, with IC50 to be 11 and 18 nM for JAK1 and JAK2 respectively and far less activity againist other kinases, including JAK3 (IC50=155 nM).
References:
A Pardanan 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, 1441–1445. [online]
JW Tyner et al. CYT387, a novel JAK2 inhibitor, induces hematologic responses and normalizes inflammatory cytokines in murine myeloproliferative neoplasms. Blood 2010, 115(25), 5232-5240. [online]
S Verstovsek. Therapeutic potential of JAK2 inhibitors. Hematology Am Soc Hematol Educ Program. 2009, 636-642. [online]
Chemical Name: N-(Cyanomethyl)-4-[2-[[4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]benzamide
|