Momelotinib (CYT387)

Catalog No.S2219 Synonyms: LM-1149 , CYT11387

Momelotinib (CYT387) Chemical Structure

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.

Size Price Stock Quantity  
In DMSO USD 220 In stock
USD 170 In stock
USD 470 In stock

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3 Customer Reviews

  • 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.

    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.

  • 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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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.
Targets
JAK1 [1] JAK2 [1] JAK3 [1]
11 nM 18 nM 155 nM
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human SET2 cells NIn2c5RRem:uaX\ldoF1cW:wIHHzd4F6 MUK3NkBp M3jCbGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1XUNkBk\WyuczDlfJBz\XO|aX7nJGpCUzJiVk[xO2YhdXW2YX70JItqdmG|ZTDh[pRmeiB5MjDodpMh[nliYXzhcYFzKGKudXWgZZN{[XluIFnDOVA:OC5{M{Kg{txO MVGxPVc3OjJ|OB?=
mouse BAF3 cells NX7leJhOWHKxbHnm[ZJifGmxbjDhd5NigQ>? NEfQXWo4OiCq NHfxbm1CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIFLBSlMh[2WubIOg[ZhxemW|c3nu[{BVTUxvSlHLNkBscW6jc3WgZYZ1\XJiN{KgbJJ{KGK7IHHsZY1ieiCkbIXlJIF{e2G7 M4nOTVE6PzZ{MkO4
human HEL 92.1.7 cells NHHJOI1Rem:uaX\ldoF1cW:wIHHzd4F6 M1r1UlczKGh? MmTuRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKRVygPVIvOS55IHPlcIx{KGW6cILld5NqdmdiSlHLNkBXPjF5RjDteZRidnRia3nuZZNmKGGodHXyJFczKGi{czDifUBidGGvYYKgZox2\SCjc4PhfUwhUUN3ME2xMlgxPCEQvF2= M3XwbVE6PzZ{MkO4

... Click to View More Cell Line Experimental Data

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]
+ Expand

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.
Cell Research:[1]
+ Expand
  • Cell lines: Ba/F3, Ba/F3-JAK2V617F and Ba/F3-MPLW515L cells
  • Concentrations: 0 to 10 μM
  • Incubation Time: 72 hours
  • Method: 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(Only for Reference)
Animal Research:[3]
+ Expand
  • Animal Models: Balb/c mice are transplanted with bone marrow transduced with a JAK2V617F retrovirus.
  • Formulation: CYT387 is dissolved 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
  • Dosages: ≤50 mg/kg
  • Administration: Administered via p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 74 mg/mL (178.54 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
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.

Chemical Information

Molecular Weight 414.46
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 Gilead Sciences November 2009 Phase 1|Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID