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JAK1 / JAK2 protein kinase inhibitor CYT 387, 5 mg  

JAK1 / JAK2 protein kinase inhibitor CYT 387, 5 mg

N-(cyanomethyl)-4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzamide

Synonyms: Momelotinib
CYT 387 is a selective and ATP-competitive Janus Kinase JAK1/JAK2 inhibitor

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PKI-CYT387-005

Availability: within 3 days

136,50 €

Background: CYT387 is a orally bioavailable ATP-competitive Janus Kinase JAK1/JAK2 inhibitor, with IC50 to be 11 and 18 nM for JAK1 and JAK2 and JAK3 (IC50=155 nM) respectively and very limited off-target effects. CYT 387 inhibits proliferation of cell lines driven by constitutively activated JAK2 or MPL signaling at nanomolar or low micromolar concentrations. Preclinical evaluation reveals that CYT 387 is able to prevent IL-6-induced phosphorylation of STAT3 and insulin-like growth factor-1-induced phosphorylation of AKT and ERK and inhibit cell cycling and induce apoptose in human myeloma cell lines.

Chemical formula: C23H22N6O2
Molecular weight: 414.46 g/mol
Purity: 99 %
Appearance: Yellow solid
Solubility: Soluble in DMSO
CAS Number: 1056634-68-4

Manufacturer:  Axon Medchem BV

PLEASE NOTE: This product is designed for research purposes and can only be delivered to academic and business customers.  

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.
 
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.
 
S Verstovsek. Therapeutic potential of JAK2 inhibitors. Hematology Am Soc Hematol Educ Program. 2009, 636-642.

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