Momelotinib sulfate
Based on 18 publication(s) in Google Scholar
Momelotinib sulfate (CYT387 sulfate salt) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, 10-fold selectivity versus JAK3 (IC50=155 nM).
For research use only. We do not sell to patients.
- Purity: 98.45%
- CAS No.: 1056636-06-6
- Formula: C23H26N6O10S2
- Molecular Weight:610.62
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Momelotinib sulfate
More- Cancer Cell. 2026 May 21:S1535-6108(26)00220-5.
- Cancer Cell. 2018 Sep 10;34(3):439-452.e6. [Abstract]
- Cancer Res. 2020 Jan 1;80(1):44-56. [Abstract]
- Nat Commun. 2025 Jul 24;16(1):6777. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Leukemia. 2012 Oct;26(10):2233-44. [Abstract]
- Metabolism. 2025 Apr 4:156259. [Abstract]
- Int J Biol Sci. 2022 Jan 1;18(2):585-598. [Abstract]
- Cell Death Dis. 2022 Dec 27;13(12):1075. [Abstract]
- Cancer Immunol Res. 2016 Jun;4(6):520-30. [Abstract]
- Cell Syst. 2018 Apr 25;6(4):424-443.e7. [Abstract]
- J Pineal Res. 2019 Apr;66(3):e12552. [Abstract]
- J Enzyme Inhib Med Chem. 2025 Dec;40(1):2488127. [Abstract]
- J Biotechnol. 2025 Mar:399:9-18. [Abstract]
- J Clin Lab Anal. 2026 Feb;40(4):e70161. [Abstract]
- Immunol Invest. 2022 Aug;51(6):1582-1597. [Abstract]
- Environ Monit Assess. 2025 Apr 10;197(5):533. [Abstract]
- bioRxiv. 2025 Oct 25.
Customer Validation & Images
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WB
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RT-PCR
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IF
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WB
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ELISA
Biological Activity
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JAK1 11 nM (IC50) |
JAK2 18 nM (IC50) |
JAK3 155 nM (IC50) |
Momelotinib sulfate (CYT387 sulfate salt) inhibits growth of Ba/F3-JAK2V617F and human erythroleukemia (HEL) cells (IC50=1.5 μM) or Ba/F3-MPLW515L cells (IC50=200 nM), but has considerably less activity against BCR-ABL harboring K562 cells (IC50=58 μM) and FLT3 mutation harboring MV4-11 cells (IC50=3 μM). Proliferation of parental Ba/F3 cells (Ba/F3-wt) stimulated with IL-3 is inhibited with an IC50 value of 1.4 μM, consistent with the established role of IL-3-dependent signaling in the parental cell line[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1056636-06-6
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Appearance Solid
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Molecular Weight 610.62
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Formula C23H26N6O10S2
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Color Light yellow to yellow
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SMILES
O=C(NCC#N)C(C=C1)=CC=C1C2=NC(NC(C=C3)=CC=C3N4CCOCC4)=NC=C2.O=S(O)(O)=O.O=S(O)(O)=O
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Synonyms
CYT387 sulfate salt
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (18)
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Journal Impact Factor
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Most Recent
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Cancer Cell
2018 Sep 10;34(3):439-452.e6. PMID: 30205046
Momelotinib sulfate purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2018 Sep 10;34(3):439-452.e6. [Abstract]
Immunoblot (IB) of the indicated proteins in A549, H2009, HCC44, and H1792 cells treated with indicated concentration of Momelotinib (MMB) for 24 hr.
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Cancer Res
Phosphorylation of RAB7 by TBK1/IKKε Regulates Innate Immune Signaling in Triple-Negative Breast Cancer. [Abstract]2020 Jan 1;80(1):44-56. PMID: 31662325
Momelotinib sulfate purchased from MedChemExpress. Usage Cited in: Cancer Res. 2020 Jan 1;80(1):44-56. [Abstract]
Immunofluorescence imaging of parental and Rab7 cell lines: WT, S72E, and S72A, treated with either 1 μM Compound 1 (6 h), 5 μM MRT67307 (8 h) or 5 μM Momelotinib (CYT387) (3 h) alone (representative, n=2; scale=10μm).
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Nat Commun
PEAK1 maintains tight junctions in intestinal epithelial cells and resists colitis by inhibiting autophagy-mediated ZO-1 degradation. [Abstract]2025 Jul 24;16(1):6777. PMID: 40707483 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Leukemia
Using combination therapy to override stromal-mediated chemoresistance in mutant FLT3-positive AML: synergism between FLT3 inhibitors, dasatinib/multi-targeted inhibitors and JAK inhibitors. [Abstract]2012 Oct;26(10):2233-44. PMID: 22469781 -
Metabolism
Propagation of senescent phenotypes by extracellular HMGB1 is dependent on its redox state. [Abstract]2025 Apr 4:156259. PMID: 40189139 -
Int J Biol Sci
Rocaglamide promotes the infiltration and antitumor immunity of NK cells by activating cGAS-STING signaling in non-small cell lung cancer. [Abstract]2022 Jan 1;18(2):585-598. PMID: 35002511
Momelotinib sulfate purchased from MedChemExpress. Usage Cited in: Int J Biol Sci. 2022 Jan 1;18(2):585-598. [Abstract]
A549, H1299, H1975, and LLC cells were treated with or without 25 nM of RocA in the presence or absence of 5 µM Momelotinib (CYT387), or 10 µM BAY11 for 24 h, and then the expressions of CCL5 and CXCL10 were analyzed by real-time PCR.
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Cell Death Dis
4EBP1 senses extracellular glucose deprivation and initiates cell death signaling in lung cancer. [Abstract]2022 Dec 27;13(12):1075. PMID: 36575176
Momelotinib sulfate purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2022 Dec 27;13(12):1075. [Abstract]
A549 cells transfected with either control siRNA or 4EBP1 siRNAs were treated with Momelotinib (CYT387) or LY3214996 for 10 h in normal or glucose starvation conditions. Western blot analysis of p-STAT3 (Y705) expression. The results showed that CYT387 and LY3214996 could inhibit the phosphorylation of STAT3. Furthermore, the increased protein levels of p-STAT3 by knocking down 4EBP1 under GS were attenuated when treating with CYT387 or LY3214996 in A549 cells.
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Cancer Immunol Res
2016 Jun;4(6):520-30. PMID: 27068336
Momelotinib sulfate purchased from MedChemExpress. Usage Cited in: Cancer Immunol Res. 2016 Jun;4(6):520-30. [Abstract]
CCL5 ELISA in 8988T-sgATG5 cells 24 h after a 60 min IL1β pulse ± 2.5 μM Momelotinib (CYT387) or ruxolitinib, mean and SD of duplicate samples shown.
Momelotinib sulfate purchased from MedChemExpress. Usage Cited in: Cancer Immunol Res. 2016 Jun;4(6):520-30. [Abstract]
H&E staining and IHC for CCL5, p62 or PD-L1 in pancreatic tissue harvested from C57/BL6 mice pretreated with vehicle control or daily Momelotinib (CYT387, 50 mg/kg; i.g.) day 1 post-cerulein. The results showed that CYT387 significantly inhibited the expression of CCL5 and PD-L1.
Momelotinib sulfate purchased from MedChemExpress. Usage Cited in: Cancer Immunol Res. 2016 Jun;4(6):520-30. [Abstract]
Inflammatory cell infiltration in pancreatic tissue from 3 random sites (200x) following vehicle (n = 4) or Momelotinib (CYT387, 50 mg/kg; i.g.; once daily for 2 days) (n = 2) treatment. Mean and SEM shown, P value calculated by Student t-test. The results demonstrated that CYT387 markedly reduced inflammatory cell infiltration following lanserin stimulation.
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Cell Syst
A Library of Phosphoproteomic and Chromatin Signatures for Characterizing Cellular Responses to Drug Perturbations. [Abstract]2018 Apr 25;6(4):424-443.e7. PMID: 29655704 -
J Pineal Res
MicroRNA-7 inhibits melatonin synthesis by acting as a linking molecule between leptin and norepinephrine signaling pathways in pig pineal gland. [Abstract]2019 Apr;66(3):e12552. PMID: 30618087 -
J Enzyme Inhib Med Chem
Discovery and biological evaluation of a novel and highly potent JAK2 inhibitor for the treatment of triple negative breast cancer. [Abstract]2025 Dec;40(1):2488127. PMID: 40298145 -
J Biotechnol
2025 Mar:399:9-18. PMID: 39824361 -
J Clin Lab Anal
The Immunoregulatory and Hematopoietic Effects of Momelotinib in a Murine Bone Marrow Failure Model. [Abstract]2026 Feb;40(4):e70161. PMID: 41552919 -
Immunol Invest
CYT387 Inhibits the Hyperproliferative Potential of Fibroblast-like Synoviocytes via Modulation of IL-6/JAK1/STAT3 Signaling in Rheumatoid Arthritis. [Abstract]2022 Aug;51(6):1582-1597. PMID: 34704880 -
Environ Monit Assess
Assessment of the physicochemical characteristics of by-products of cassava processing and their effects on biodiversity. [Abstract]2025 Apr 10;197(5):533. PMID: 40208441 -
Solvent & Solubility
DMSO : 100 mg/mL (163.77 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 100 mg/mL (163.77 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 3 mg/mL (4.91 mM); Clear solution
This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 3 mg/mL (4.91 mM); Clear solution
This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (163.77 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Protocol
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[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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. TheTEL/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 h at 37°C with 5% CO2[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[2]
On day 32 after bone marrow transplantation (when all mice exhibit severe leukocytosis and erythrocytosis), mice are assigned to 3 groups such that each group has equivalent average body weight and blood counts. Momelotinib (CYT387) is dissolved in NMP (120 mg/mL final; 1-methyl-2-pyrrolidinone, Chromasolv Plus). Subsequently, the Momelotinib/NMP mix is diluted with 0.14M Captisol to a concentration of 6 mg/mL and further diluted with 0.1M Captisol to a final concentration of 4 mg/mL. All 3 groups of mice (n=12 per group) are administered Momelotinib (CYT387) by oral gavage twice daily at 10- to 12-hour intervals from day 34 after bone marrow transplantation to day 82 (end of experiment). Mice receive NMP/Captisol without Momelotinib (CYT387) (0 mg/kg group), 25 mg/kg Momelotinib, or 50 mg/kg Momelotinib. At day 82 after bone marrow transplantation, all mice are euthanized for analysis except for 2 mice each from the 50 mg/kg and 25 mg/kg groups, which are taken off Momelotinib (CYT387) treatment and followed for 45 additional days. For assessment of the effects of Momelotinib (CYT387) on normal blood counts, naive Balb/c mice are administered vehicle control, 50 mg/kg, or 100 mg/kg Momelotinib (CYT387) in an identical fashion as described for the bone marrow transplant experimental mouse cohort. Peripheral blood is drawn at day 14, 28, 42, and 56 and levels of red cells, white cells, reticulocytes, granulocytes, lymphocytes, and monocytes are analyzed.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (283 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Pardanani A, et al. CYT387, a selective JAK1/JAK2 inhibitor: in vitro assessment of kinase selectivity and preclinical studies using cell lines and primary cells from polycythemia vera patients. Leukemia, 2009, 23(8), 1441-1445. [Content Brief]
[2]. Tyner JW, et al. CYT387, a novel JAK2 inhibitor, induces hematologic responses and normalizes inflammatory cytokines in murine myeloproliferative neoplasms. Blood, 2010, 115(25), 5232-5240. [Content Brief]
[3]. Burns CJ, et al. Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs). Bioorg Med Chem Lett. 2009 Oct 15;19(20):5887-92. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 1.6377 mL | 8.1884 mL | 16.3768 mL | 40.9420 mL |
| 5 mM | 0.3275 mL | 1.6377 mL | 3.2754 mL | 8.1884 mL | |
| 10 mM | 0.1638 mL | 0.8188 mL | 1.6377 mL | 4.0942 mL | |
| 15 mM | 0.1092 mL | 0.5459 mL | 1.0918 mL | 2.7295 mL | |
| 20 mM | 0.0819 mL | 0.4094 mL | 0.8188 mL | 2.0471 mL | |
| 25 mM | 0.0655 mL | 0.3275 mL | 0.6551 mL | 1.6377 mL | |
| 30 mM | 0.0546 mL | 0.2729 mL | 0.5459 mL | 1.3647 mL | |
| 40 mM | 0.0409 mL | 0.2047 mL | 0.4094 mL | 1.0235 mL | |
| 50 mM | 0.0328 mL | 0.1638 mL | 0.3275 mL | 0.8188 mL | |
| 60 mM | 0.0273 mL | 0.1365 mL | 0.2729 mL | 0.6824 mL | |
| 80 mM | 0.0205 mL | 0.1024 mL | 0.2047 mL | 0.5118 mL | |
| 100 mM | 0.0164 mL | 0.0819 mL | 0.1638 mL | 0.4094 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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