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.

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In DMSO USD 220 In stock
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Cited by 20 Publications

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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]
(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 MUXQdo9tcW[ncnH0bY9vKGG|c3H5 M{jtTFczKGh? NVLv[|ZiSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTSXQzKGOnbHzzJIV5eHKnc4PpcochUkGNMjDWOlE4TiCvdYThcpQhc2mwYYPlJIFnfGW{IEeyJIhzeyCkeTDhcIFu[XJiYnz1[UBie3OjeTygTWM2OD1yLkKzNkDPxE1? NXniT5hjOTl5NkKyN|g>
mouse BAF3 cells NHvnPWJRem:uaX\ldoF1cW:wIHHzd4F6 NUCxSHVuPzJiaB?= NH3UblZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIFLBSlMh[2WubIOg[ZhxemW|c3nu[{BVTUxvSlHLNkBscW6jc3WgZYZ1\XJiN{KgbJJ{KGK7IHHsZY1ieiCkbIXlJIF{e2G7 NHfUT4YyQTd4MkKzPC=>
human HEL 92.1.7 cells NX7re|JrWHKxbHnm[ZJifGmxbjDhd5NigQ>? NHG4T|M4OiCq MYjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiHTDC5Nk4yNjdiY3XscJMh\XiycnXzd4lv\yCMQVuyJHY3OTeIIH31eIFvfCCtaX7hd4Uh[W[2ZYKgO|IhcHK|IHL5JIFt[W2jcjDicJVmKGG|c3H5MEBKSzVyPUGuPFA1KM7:TR?= NYXSdm5ZOTl5NkKyN|g>

... Click to View More Cell Line Experimental Data
Assay
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.

26625308
Immunofluorescence
p62 / pS6 ; 

PubMed: 29138276     


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

29138276
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.

20385788
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]
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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.
  • 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 Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing. 		30 mg/mL

* 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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID