Home JAK/STAT JAK inhibitor - Apoptosis related activator - Autophagy activator Momelotinib (CYT387) For research use only.

Momelotinib (CYT387)

Synonyms: LM-1149 , CYT11387

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.

Momelotinib (CYT387) Chemical Structure

Momelotinib (CYT387) Chemical Structure

CAS No. 1056634-68-4

Purity & Quality Control

Momelotinib (CYT387) Related Products

Signaling Pathway

JAK Signaling Pathways

JAK Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SET2 Antiproliferative assay 72 hrs Antiproliferative activity against human SET2 cells expressing JAK2 V617F mutant kinase after 72 hrs by alamar blue assay, IC50=0.232μM. 19762238
BAF3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BAF3 cells expressing TEL-JAK2 kinase after 72 hrs by alamar blue assay, IC50=0.798μM. 19762238
CTLL-2 Antiproliferative assay 72 hrs Antiproliferative activity against IL-2-stimulated mouse CTLL-2 cells expressing JAK1/JAK3 after 72 hrs by alamar blue assay, IC50=1.249μM. 19762238
BAF3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BAF3 cells expressing wild type JAK2 kinase after 72 hrs by alamar blue assay in presence of IL-3, IC50=1.43μM. 19762238
HEL 92.1.7 Antiproliferative assay 72 hrs Antiproliferative activity against human HEL 92.1.7 cells expressing JAK2 V617F mutant kinase after 72 hrs by alamar blue assay, IC50=1.804μM. 19762238
HEL Antiproliferative assay 48 hrs Antiproliferative activity against human HEL cells after 48 hrs by CCK-8 assay, IC50=2.3μM. 29940115
BAF3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BAF3 cells expressing TEL-JAK3 kinase after 72 hrs by alamar blue assay, IC50=2.425μM. 19762238
K562 Antiproliferative assay 48 hrs Antiproliferative activity against human K562 cells after 48 hrs by CCK-8 assay, IC50=6.5μM. 29940115
HL60 Antiproliferative assay 48 hrs Antiproliferative activity against human HL60 cells after 48 hrs by CCK-8 assay, IC50=8.3μM. 29940115
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
BAF3 Function assay Inhibition of JAK2 V617F mutant in mouse BAF3 cells, IC50=1.5μM. ChEMBL
Click to View More Cell Line Experimental Data

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.
Targets
JAK1 [1]
(Cell-free assay)		 JAK2 [1]
(Cell-free assay)		 JAK3 [1]
(Cell-free assay)
11 nM 18 nM 155 nM
In vitro
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]
Kinase Assay 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 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
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-JAK2 / JAK2 / p-STAT3 / STAT3 p-Src / Src 26625308
Immunofluorescence p62 / pS6 29138276
Growth inhibition assay Cell viability 20385788
In Vivo
In vivo In a murine MPN model, CYT387 normalizes white cell counts, hematocrit, spleen size, and restores physiologic levels of inflammatory cytokines. [3]
Animal Research Animal Models Balb/c mice are transplanted with bone marrow transduced with a JAK2V617F retrovirus.
Dosages ≤50 mg/kg
Administration Administered via p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01236638 Completed
Primary Myelofibrosis|Post-Polycythemia Vera Myelofibrosis|Post-Essential Thrombocythemia Myelofibrosis
Sierra Oncology LLC - a GSK company
 November 2010 Phase 2
NCT00935987 Completed
Primary Myelofibrosis|Post-Polycythemia Vera Myelofibrosis|Post-Essential Thrombocythemia Myelofibrosis
Sierra Oncology LLC - a GSK company
 November 2009 Phase 1|Phase 2

Chemical Information & Solubility

Molecular Weight 414.46 Formula

C23H22N6O2
CAS No. 1056634-68-4 SDF Download Momelotinib (CYT387) SDF
Smiles C1COCCN1C2=CC=C(C=C2)NC3=NC=CC(=N3)C4=CC=C(C=C4)C(=O)NCC#N
Storage (From the date of receipt) 3 years -20°C(in the dark) powder

In vitro
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DMSO : 83 mg/mL ( (200.26 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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