Momelotinib (CYT387)
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.
4 Customer Reviews
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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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Shown are WT pan T cells (both CD4＋and CD8＋ T cells; CD4－T cells are CD8＋T cells) after drug treatment.
Blood 2012 120(19), 4093-103. Momelotinib (CYT387) purchased from Selleck.
Percent pJAK2 and pSTAT5 for each cell line and inhibitor condition are displayed relative to mean basal phosphoprotein levels of control CD45+14+18+ myeloid cells. Experiments were performed in triplicate. Statistical analyses were performed with ANOVA and the Dunnett post-test for multiple comparisons. *p < 0.05, **p < 0.01, ***p < 0.001, ****p < 0.0001
Leukemia, 2018, doi:10.1038/s41375-018-0169-y. Momelotinib (CYT387) purchased from Selleck.
Purity & Quality Control
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Biological Activity
| 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. | ||||||||||||||||||||||||||||||
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| In vitro |
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. [1] 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. [2] |
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| Cell Data |
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| In vivo | In a murine MPN model, CYT387 normalizes white cell counts, hematocrit, spleen size, and restores physiologic levels of inflammatory cytokines. [3] |
Protocol
| Kinase Assay:[1] |
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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. |
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| Cell Research:[1] |
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| Animal Research:[3] |
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Solubility (25°C)
| In vitro | DMSO | 74 mg/mL (178.54 mM) |
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| Water | Insoluble | |
| Ethanol | Insoluble | |
| In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 30% PEG400+0.5% Tween80+5% propylene glycol For best results, use promptly after mixing. |
30 mg/mL |
* 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.
Chemical Information
| Molecular Weight | 414.46 |
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| Formula | C23H22N6O2 |
| CAS No. | 1056634-68-4 |
| Storage | powder |
| in solvent | |
| 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 | Sierra Oncology Inc. | November 2009 | Phase 1|Phase 2 |
| NCT00935987 | Completed | Primary Myelofibrosis|Post-Polycythemia Vera Myelofibrosis|Post-Essential Thrombocythemia Myelofibrosis | Sierra Oncology Inc. | November 2009 | Phase 1|Phase 2 |
Tech Support
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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