Cat. No. Name Size Price Add Cart
KI0095CYT38710 mg$272
CYT38750 mg$752
CYT387200 mg$2032

Chemical Characteristic

Product NameCYT387
SynonymsMomelotinib
CAS No.1056634-68-4
Molecular Weight 414.46
FormulaC23H22N6O2
Chemical NameN-(cyanomethyl)-4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzamide
SmilesC(=O)(c1ccc(cc1)c1nc(ncc1)Nc1ccc(cc1)N1CCOCC1)NCC#N
Chemical Structure

Biological activities

CYT387 is an ATP-competitive inhibitor of JAK1 and JAK2 with IC50 of 11 and 18 nM, respectively. CYT387 inhibits proliferation of JAK2V617F mutation harboring human erythroleukemia (HEL) cells as well as Ba/F3-JAK2V617F cells with an IC50 of approximately 1.5 µM. CYT387 also inhibits proliferation of parental Ba/F3 cells (Ba/F3-wt) stimulated with IL-3 with an IC50 of 1.4 µM, consistent with the established role of IL-3-dependent signaling in the parental cell line. CYT387 inhibits phosphorylation of signal transducer and activator transcription (STAT) -5 and -3 in HEL cells. In the presence of erythropoietin, CYT387 inhibits erythroid colony growth from JAK2V617F-positive polycythemia vera (PV) patients with similar potency. [1] CYT387 inhibits the activity of recombinant JAK3, and tyrosine kinase 2 (TYK2) kinase domains with IC50 of 155, and 17 nM, respectively. CYT387 selectively inhibits JAK2-dependent cell lines (HEL, JAK2V617F) with IC50 range between 0.5 and 1.5 µM. 0.3 µM CYT387 can inhibit phosphorylation of extracellular signal-regulated kinase 1/2 (ERK1/2) and signal transducer and activator of transcription 5 (STAT5). CYT387 restores hematopoietic lineage composition, but JAK2V617F-expressing cells persist. CYT387 is ef?cacious in an in vivo model of JAK2V617F-dependent myeloproliferative neoplasms (MPN), in which lethally irradiated Balb/c mice are transplanted with bone marrow transduced with a JAK2V617F retrovirus. Mice with JAK2V617F-induced disease exhibit a complex perturbation of cytokine and chemokine expression that is at least partially normalized by CYT387. [2]

Protocols

CYT387 is diluted in culture medium and stock solution is made in DMSO. [1]

References

[1] 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.
[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.

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