Catalog No.S2219 Synonyms: LM-1149 , CYT11387
Molecular Weight(MW): 414.46
Momelotinib (CYT387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, ~10-fold selectivity versus JAK3. Phase 3.
Cited by 6 Publications
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IL-6- supported INA-6 cells were treated with the JAK inhibitors ruxolitinib (Rux; 10 nM) or CYT387 (CYT; 50 nM) for 1 hour and assessed for inhibition of STAT3 phosphorylation by immunoblotting.
J Clin Invest 2014 10.1172/JCI69094. Momelotinib (CYT387) purchased from Selleck.
HEL cells, expressing the Jak2-V617F mutant and showing constitutive activation of STAT5, were treated for 3h with Cyt387 at the indicated concentrations. Cells lysates were then subjected to SDS-PAGE and Western blotting. The Blots were detected with the indicated fluorescent antibodies using the LI-COR Biosciences detection system.
2014 Dr. Claude Haan and Catherine Rolvering from University of Luxembourg. Momelotinib (CYT387) purchased from Selleck.
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|Description||Momelotinib (CYT387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, ~10-fold selectivity versus JAK3. Phase 3.|
CYT387 inhibits the proliferation of parental Ba/F3 cells (Ba/F3-wt) stimulated by IL-3 with IC50 of 1400 nM. Furthermore, CYT387 also causes the inhibition of cell proliferation in cell lines constitutively activated by JAK2 or MPL signaling, including Ba/F3-MPLW515L cells, CHRF-288-11 cells and Ba/F3-TEL-JAK2 cells with IC50 of 200 nM, 1 nM and 700 nM, respectively. In addition, CYT387 has been shown to inhibit erythroid colony growth in vitro from JAK2V617F-positive PV patients with similar potency with IC50 of 2μ-4 μM.  A recent study shows that CYT387 inhibits PI3K/AKT and Ras/MAPK signaling induced by IL-6 and IGF-1. Moreover, CYT387 induces apoptosis as a single agent and synergizes with the conventional anti-MM therapies bortezomib and melphalan in primary multiple myeloma (MM) cells. 
|In vivo||In a murine MPN model, CYT387 normalizes white cell counts, hematocrit, spleen size, and restores physiologic levels of inflammatory cytokines. |
Cell-free kinase activity assays:Glutathione-S-transferase (GST)-tagged JAK kinase domains expressed in insect cells are purified before use in a peptide substrate phosphorylation assay. Assays are carried out in 384-well optiplates using an Alphascreen Protein Tyrosine Kinase P100 detection kit and a PerkinElmer Fusion Alpha instrument.
|In vitro||DMSO||74 mg/mL (178.54 mM)|
|In vivo||30% PEG400+0.5% Tween80+5% propylene glycol||30 mg/mL|
* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
|Synonyms||LM-1149 , CYT11387|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT00935987||Completed||Primary Myelofibrosis|Post-Polycythemia Vera Myelofibrosis|Post-Essential Thrombocythemia Myelofibrosis||Gilead Sciences||November 2009||Phase 1|Phase 2|
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