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    Momelotinib (LM1149; CYT387; CYT11387)
    Momelotinib (LM1149; CYT387; CYT11387)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0323
    CAS #: 1056634-68-4Purity ≥98%

    Description: Momelotinib (formerly CYT-387; CYT-11387; LM-1149), an aminopyrimidine analog, is a novel, potent and ATP-competitive inhibitor of Janus kinases (JAK1/2) with potential antitumor and anti-inflammatory activity. It inhibits JAK1/2 with IC50s of 11 nM/18 nM, and shows ~10-fold selectivity for JAK1/2 over JAK3. CYT 387 is currently undergoing Phase I/II clinical trials for treating myelofibrosis. Momelotinib shows potent in vitro antiproliferative activity and high in vivo antitumor efficacy. It was discovered by high-throughput enzyme and cell-based screening along with the optimization using structure-guided medicinal chemistry. 

    References: Leukemia. 2009 Aug;23(8):1441-5; Leukemia. 2011 Dec;25(12):1891-9; Blood. 2010 Jun 24;115(25):5232-40.

    Related CAS: 1056636-07-7 (Momelotinib Mesylate); 1056636-06-6 (Momelotinib sulfate); 1380317-28-1 (HCl); 1056634-68-4 (free base) 

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    Molecular Weight (MW)414.46
    FormulaC23H22N6O2
    CAS No.1056634-68-4  (free base);
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 74 mg/mL (178.5 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/mL 
    Synonyms

    LM-1149 , CYT-11387; LM 1149 , CYT 11387; LM1149 , CYT11387;  CYT-387; Momelotinib; Momelotinib free base; CYT387;  CYT 387

    Chemical Name: N-(cyanomethyl)-4-(2-((4-morpholinophenyl)amino)pyrimidin-4-yl)benzamide.

    InChi Key: ZVHNDZWQTBEVRY-UHFFFAOYSA-N

    InChi Code: InChI=1S/C23H22N6O2/c24-10-12-25-22(30)18-3-1-17(2-4-18)21-9-11-26-23(28-21)27-19-5-7-20(8-6-19)29-13-15-31-16-14-29/h1-9,11H,12-16H2,(H,25,30)(H,26,27,28)

    SMILES Code: O=C(NCC#N)C1=CC=C(C2=NC(NC3=CC=C(N4CCOCC4)C=C3)=NC=C2)C=C1 


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    In Vitro

    In vitro activity: 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.


    Kinase Assay: 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.


    Cell Assay: Ba/F3 cells expressing JAK2V617F (Ba/F3-JAK2V617F) and MPLW515L (Ba/F3-MPLW515L) mutants, as well as CHRF-288-11 (JAK2T875N) and CMK (JAK3A572V) cells are used. The TEL/JAK2 and TEL/JAK3 fusions are generated and introduced into Ba/F3 murine cells. The TEL/JAK2- or TEL/JAK3-transfected cells are cultured in Dulbecco's modified Eagle's medium (DMEM) containing 10% fetal calf serum (FCS). Ba/F3 wild-type cells are cultured in RPMI containing 10% FCS supplemented with 5 ng/mL murine IL-3. Proliferation is measured using the Alamar Blue assay after incubating for 72 hours at 37 °C with 5% CO2

    In VivoIn a murine MPN model, CYT387 normalizes white cell counts, hematocrit, spleen size, and restores physiologic levels of inflammatory cytokines.
    Animal modelBalb/c mice are transplanted with bone marrow transduced with a JAK2V617F retrovirus.
    Formulation & DosageDissolved in NMP (120 mg/mL final; 1-methyl-2-pyrrolidinone, Chromasolv Plus). Subsequently, the CYT387/NMP mix is diluted with 0.14 M Captisol to a concentration of 6 mg/mL and further diluted with 0.1M Captisol to a final concentration of 4 mg; 50 mg daily; Oral gavage
    References

    Leukemia. 2009 Aug;23(8):1441-5; Leukemia. 2011 Dec;25(12):1891-9; Blood. 2010 Jun 24;115(25):5232-40.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Momelotinib (CYT387)


    Momelotinib (CYT387)

    Momelotinib (CYT387)

    Effect of CYT387 on cytokine concentrations during MPN in vivo. Blood. 2010 Jun 24;115(25):5232-40.

    Momelotinib (CYT387)

    Efficacy of CYT387 against JAK2-dependent malignancy in vivo. Blood. 2010 Jun 24;115(25):5232-40. 


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