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Momelotinib (CYT387)

Name: Momelotinib (CYT387)
Brand: Selleck Chemicals
SKU: S2219
Rating: 5 (47 reviews)

Synonyms: LM-1149 , CYT11387

Catalog No.S2219 Purity: 99.75%

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

CAS: 1056634-68-4

Selleck's Momelotinib (CYT387) has been cited by 47 publications

Purity & Quality Control

Batch: Purity: 99.75%

99.75

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Cell Data

Cell Lines	Assay Type	Incubation Time	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

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
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 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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
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

References

Chemical lnformation & 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	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years -20°C(in the dark) powder		1 month-20°Cin solvent

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble

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In vivo
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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.

Handling Instructions

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