Momelotinib (CYT387)

For research use only.

Catalog No.S2219 Synonyms: LM-1149 , CYT11387

33 publications

Momelotinib (CYT387) Chemical Structure

CAS No. 1056634-68-4

Momelotinib (CYT387, LM-1149 , CYT11387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, ~10-fold selectivity versus JAK3. Momelotinib (CYT387) induces apoptosis and autophagy. Phase 3.

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Selleck's Momelotinib (CYT387) has been cited by 33 publications

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Biological Activity

Description Momelotinib (CYT387, LM-1149 , CYT11387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, ~10-fold selectivity versus JAK3. Momelotinib (CYT387) induces apoptosis and autophagy. Phase 3.
JAK1 [1]
(Cell-free assay)
JAK2 [1]
(Cell-free assay)
JAK3 [1]
(Cell-free assay)
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 Mn7GVJJwdGmoZYLheIlwdiCjc4PhfS=> MWq3NkBp M4LDVGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1XUNkBk\WyuczDlfJBz\XO|aX7nJGpCUzJiVk[xO2YhdXW2YX70JItqdmG|ZTDh[pRmeiB5MjDodpMh[nliYXzhcYFzKGKudXWgZZN{[XluIFnDOVA:OC5{M{Kg{txO NYDpfHQ3OTl5NkKyN|g>
mouse BAF3 cells NVHtdXQzWHKxbHnm[ZJifGmxbjDhd5NigQ>? M2TNWlczKGh? NYPzV2dOSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBud3W|ZTDCRWY{KGOnbHzzJIV5eHKnc4PpcochXEWOLVrBT|Ihc2mwYYPlJIFnfGW{IEeyJIhzeyCkeTDhcIFu[XJiYnz1[UBie3OjeR?= MV[xPVc3OjJ|OB?=
human HEL 92.1.7 cells NU\Lfo53WHKxbHnm[ZJifGmxbjDhd5NigQ>? M1nodVczKGh? NEG5To1CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjFUEA6Oi5zLkegZ4VtdHNiZYjwdoV{e2mwZzDKRWszKFZ4MUfGJI12fGGwdDDrbY5ie2ViYX\0[ZIhPzJiaILzJIJ6KGGuYX3hdkBjdHWnIHHzd4F6NCCLQ{WwQVEvQDB2IN88US=> MnzuNVk4PjJ{M{i=

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
p-JAK2 / JAK2 / p-STAT3 / STAT3 ; 

PubMed: 26625308     

RCC cell lines were treated for 24 hours with the indicated concentrations of CYT387, and lysates were probed with the indicated antibodies. Actin was used as loading control.

p-Src / Src ; 

PubMed: 26625308     

RCC cells were treated with 100 nM of dasatinib and 2 μM of CYT387, alone, in combination or DMSO for 24 hours and lysates were probed with the indicated antibodies.

p62 / pS6 ; 

PubMed: 29138276     

ACHN cells were grown on coverslips, treated with CYT387 for 24 h, and stained p62 and p-S6. 

Growth inhibition assay
Cell viability; 

PubMed: 20385788     

Ba/F3-EpoR parental (cultured in media supplemented with 3 U/mL erythropoietin) or Ba/F3-EpoR-JAK2(V617F) cells (cultured in the absence of exogenous cytokines) were plated in 96-well plates over a dose gradient of CYT387 for 3 days at which point cell viability was measured with an MTS tetrazolium salt assay. Values represent mean ± SEM. n = 3; *P < .05.

In vivo In a murine MPN model, CYT387 normalizes white cell counts, hematocrit, spleen size, and restores physiologic levels of inflammatory cytokines. [3]


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.
Cell Research:[1]
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  • 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]
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  • Animal Models: Balb/c mice are transplanted with bone marrow transduced with a JAK2V617F retrovirus.
  • 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 Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+40%PEG 300+ 3% Tween80 + ddH2O
For best results, use promptly after mixing.

* 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


CAS No. 1056634-68-4
Storage powder
in solvent
Synonyms LM-1149 , CYT11387
Smiles C1COCCN1C2=CC=C(C=C2)NC3=NC=CC(=N3)C4=CC=C(C=C4)C(=O)NCC#N

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID