Cat. No.: HY-10961

Momelotinib

Name: Momelotinib
Brand: MedChemExpress
SKU: HY-10961
Price: 92.00 USD
Availability: InStock
Rating: 5 (19 reviews)

(Synonyms: CYT387)

19 Cited Publications

고객리뷰

Based on 19 publication(s) in Google Scholar

Momelotinib (CYT387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC₅₀a of 11 nM and 18 nM,respectively. CYT387 shows much less activity against JAK3.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

Purity : 98.73%
CAS No.: 1056634-68-4
화학식: C₂₃H₂₂N₆O₂
분자량:414.46

보관:

Please store the product under the recommended conditions in the Certificate of Analysis.

Momelotinib Chemical Structure

CAS No.: 1056634-68-4

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (19)
용액&용해도
- In Vitro
- In Vivo
순도&문서
References
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

Momelotinib (CYT387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC₅₀a of 11 nM and 18 nM,respectively. CYT387 shows much less activity against JAK3.

IC₅₀ & Target

^[1]

JAK1

11 nM (IC₅₀)

JAK2

18 nM (IC₅₀)

JAK3

155 nM (IC₅₀)

All JAK Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	1424 nM Compound: CYT387	Antiproliferative activity against IL-6 stimulated wild type mouse BaF3 cells measured after 72 hrs by Alamar blue staining based analysis Antiproliferative activity against IL-6 stimulated wild type mouse BaF3 cells measured after 72 hrs by Alamar blue staining based analysis	[PMID: 19295546]
BaF3	IC₅₀	1500 nM Compound: CYT387	Antiproliferative activity against mouse BaF3 cells harboring JAK2V617F mutant measured after 72 hrs by Alamar blue staining based analysis Antiproliferative activity against mouse BaF3 cells harboring JAK2V617F mutant measured after 72 hrs by Alamar blue staining based analysis	[PMID: 19295546]
BaF3	IC₅₀	200 nM Compound: CYT387	Antiproliferative activity against mouse BaF3 cells harboring MPLW515L measured after 72 hrs by Alamar blue staining based analysis Antiproliferative activity against mouse BaF3 cells harboring MPLW515L measured after 72 hrs by Alamar blue staining based analysis	[PMID: 19295546]
BaF3	IC₅₀	2348 nM Compound: CYT387	Antiproliferative activity against mouse BaF3 cells harboring TEL-JAK3 measured after 72 hrs by Alamar blue staining based analysis Antiproliferative activity against mouse BaF3 cells harboring TEL-JAK3 measured after 72 hrs by Alamar blue staining based analysis	[PMID: 19295546]
BaF3	IC₅₀	724 nM Compound: CYT387	Antiproliferative activity against mouse BaF3 cells harboring TEL-JAK2 measured after 72 hrs by Alamar blue staining based analysis Antiproliferative activity against mouse BaF3 cells harboring TEL-JAK2 measured after 72 hrs by Alamar blue staining based analysis	[PMID: 19295546]
BaF3	IC₅₀	1430 nM Compound: 28	Antiproliferative activity against mouse BAF3 cells expressing wild type JAK2 kinase after 72 hrs by alamar blue assay in presence of IL-3 Antiproliferative activity against mouse BAF3 cells expressing wild type JAK2 kinase after 72 hrs by alamar blue assay in presence of IL-3	[PMID: 19762238]
BaF3	IC₅₀	2425 nM Compound: 28	Antiproliferative activity against mouse BAF3 cells expressing TEL-JAK3 kinase after 72 hrs by alamar blue assay Antiproliferative activity against mouse BAF3 cells expressing TEL-JAK3 kinase after 72 hrs by alamar blue assay	[PMID: 19762238]
BaF3	IC₅₀	798 nM Compound: 28	Antiproliferative activity against mouse BAF3 cells expressing TEL-JAK2 kinase after 72 hrs by alamar blue assay Antiproliferative activity against mouse BAF3 cells expressing TEL-JAK2 kinase after 72 hrs by alamar blue assay	[PMID: 19762238]
BaF3	IC₅₀	1.5 μM Compound: 9, CYT387	Inhibition of JAK2 V617F mutant in mouse BAF3 cells Inhibition of JAK2 V617F mutant in mouse BAF3 cells	10.1039/C1MD00175B
CMK	IC₅₀	700 nM Compound: CYT387	Antiproliferative activity against human CMK cells harboring JAK3A572V mutant measured after 72 hrs by Alamar blue staining based analysis Antiproliferative activity against human CMK cells harboring JAK3A572V mutant measured after 72 hrs by Alamar blue staining based analysis	[PMID: 19295546]
HCC1143	IC₅₀	5 μM Compound: 91; CYT387	Anticancer activity against human HCC1143 cells assessed as cell growth inhibition Anticancer activity against human HCC1143 cells assessed as cell growth inhibition	[PMID: 33650861]
HCC1187	IC₅₀	1 μM Compound: 91; CYT387	Anticancer activity against human HCC1187 cells assessed as cell growth inhibition Anticancer activity against human HCC1187 cells assessed as cell growth inhibition	[PMID: 33650861]
HCC70	IC₅₀	10 μM Compound: 91; CYT387	Anticancer activity against human HCC70 cells assessed as cell growth inhibition Anticancer activity against human HCC70 cells assessed as cell growth inhibition	[PMID: 33650861]
HEL	IC₅₀	1804 nM Compound: 28	Antiproliferative activity against human HEL 92.1.7 cells expressing JAK2 V617F mutant kinase after 72 hrs by alamar blue assay Antiproliferative activity against human HEL 92.1.7 cells expressing JAK2 V617F mutant kinase after 72 hrs by alamar blue assay	[PMID: 19762238]
HEL	IC₅₀	2.3 μM Compound: 1; CYT-387	Antiproliferative activity against human HEL cells after 48 hrs by CCK-8 assay Antiproliferative activity against human HEL cells after 48 hrs by CCK-8 assay	[PMID: 29940115]
HEL	IC₅₀	0.95 μM Compound: 1	Antiproliferative activity against HEL cells Antiproliferative activity against HEL cells	[PMID: 38838918]
HL-60	IC₅₀	8.3 μM Compound: 1; CYT-387	Antiproliferative activity against human HL60 cells after 48 hrs by CCK-8 assay Antiproliferative activity against human HL60 cells after 48 hrs by CCK-8 assay	[PMID: 29940115]
K562	IC₅₀	58000 nM Compound: CYT387	Antiproliferative activity against human K562 cells measured after 72 hrs by Alamar blue staining based analysis Antiproliferative activity against human K562 cells measured after 72 hrs by Alamar blue staining based analysis	[PMID: 19295546]
K562	IC₅₀	>20000 nM Compound: 28	Antiproliferative activity against human K562 cells after 72 hrs by alamar blue assay Antiproliferative activity against human K562 cells after 72 hrs by alamar blue assay	[PMID: 19762238]
K562	IC₅₀	6.5 μM Compound: 1; CYT-387	Antiproliferative activity against human K562 cells after 48 hrs by CCK-8 assay Antiproliferative activity against human K562 cells after 48 hrs by CCK-8 assay	[PMID: 29940115]
K562	IC₅₀	4.7 μM Compound: 1	Antiproliferative activity against human K562 cells Antiproliferative activity against human K562 cells	[PMID: 38838918]
MDA-MB-231	IC₅₀	1 μM Compound: 91; CYT387	Anticancer activity against human MDA-MB-231 cells assessed as cell growth inhibition Anticancer activity against human MDA-MB-231 cells assessed as cell growth inhibition	[PMID: 33650861]
MDA-MB-468	IC₅₀	1 μM Compound: 91; CYT387	Anticancer activity against human MDA-MB-468 cells assessed as cell growth inhibition Anticancer activity against human MDA-MB-468 cells assessed as cell growth inhibition	[PMID: 33650861]
MV4-11	IC₅₀	3000 nM Compound: CYT387	Antiproliferative activity against human MV4-11 cells measured after 72 hrs by Alamar blue staining based analysis Antiproliferative activity against human MV4-11 cells measured after 72 hrs by Alamar blue staining based analysis	[PMID: 19295546]
SET-2	IC₅₀	232 nM Compound: 28	Antiproliferative activity against human SET2 cells expressing JAK2 V617F mutant kinase after 72 hrs by alamar blue assay Antiproliferative activity against human SET2 cells expressing JAK2 V617F mutant kinase after 72 hrs by alamar blue assay	[PMID: 19762238]
THP-1	IC₅₀	8.8 μM Compound: 1	Antiproliferative activity against human THP-1 cells Antiproliferative activity against human THP-1 cells	[PMID: 38838918]

In Vitro

Momelotinib (CYT387) inhibits the proliferation of parental Ba/F3 cells (Ba/F3-wt) stimulated by IL-3 with IC₅₀ of 1400 nM. Furthermore, Momelotinib (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, Momelotinib (CYT387) has been shown to inhibit erythroid colony growth in vitro from JAK2V617F-positive PV patients with similar potency with IC₅₀ of 2 μM-4 μM^[1]. Momelotinib (CYT387) inhibits PI3K/AKT and Ras/MAPK signaling induced by IL-6 and IGF-1. Moreover, Momelotinib (CYT387) induces apoptosis as a single agent and synergizes with the conventional anti-MM therapies PS-341 and L-PAM in primary multiple myeloma (MM) cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991			2011-05	PHASE1

Chemical Information

CAS No. 1056634-68-4
Appearance Solid
분자량 414.46
화학식 C₂₃H₂₂N₆O₂
Color Light yellow to yellow
SMILES

O=C(C1=CC=C(C2=NC(NC3=CC=C(N4CCOCC4)C=C3)=NC=C2)C=C1)NCC#N
Synonyms

CYT387
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (19)

All IFRT-PCRWBELISAHistological Imaging/StainingIn Vivo Efficacy Study

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Journal Impact Factor

Cancer Cell

2026 May 21:S1535-6108(26)00220-5. PMID: 42167227
Cancer Cell

Overcoming Resistance to Dual Innate Immune and MEK Inhibition Downstream of KRAS. [Abstract]

2018 Sep 10;34(3):439-452.e6. PMID: 30205046

Momelotinib 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.
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 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).
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
Metabolism

Propagation of senescent phenotypes by extracellular HMGB1 is dependent on its redox state. [Abstract]

2025 Jul:168:156259. PMID: 40189139
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
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 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.
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 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.
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
Cancer Immunol Res

Autophagy Inhibition Dysregulates TBK1 Signaling and Promotes Pancreatic Inflammation. [Abstract]

2016 Jun;4(6):520-30. PMID: 27068336

Momelotinib 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 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 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.
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
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 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

Interferon inhibitors increase rAAV production in HEK293 cells. [Abstract]

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
Biomed Pharmacother

2026 Sep:202:119803. PMID: 42537395
bioRxiv

2025 Oct 25.

용액&용해도

In Vitro:

DMSO : 10 mg/mL (24.13 mM; ultrasonic and warming and adjust pH to 3 with HCl and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4128 mL

12.0639 mL

24.1278 mL

5 mM

0.4826 mL

2.4128 mL

4.8256 mL

10 mM

0.2413 mL

1.2064 mL

2.4128 mL

몰농도 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 1 mg/mL (2.41 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 1 mg/mL (2.41 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

In Vivo Dissolution Calculator

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The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (396 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
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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]. Monaghan KA, et al. The novel JAK inhibitor CYT387 suppresses multiple signalling pathways, prevents proliferation and induces apoptosis in phenotypically diverse myeloma cells. Leukemia, 2011, 25(12), 1891-1899. [Content Brief]

[3]. 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]

[4]. Kitajima S, et al.Overcoming Resistance to Dual Innate Immune and MEK Inhibition Downstream of KRAS.Cancer Cell. 2018 Sep 10;34(3):439-452.e6. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.4128 mL	12.0639 mL	24.1278 mL	60.3195 mL
	5 mM	0.4826 mL	2.4128 mL	4.8256 mL	12.0639 mL
	10 mM	0.2413 mL	1.2064 mL	2.4128 mL	6.0319 mL
	15 mM	0.1609 mL	0.8043 mL	1.6085 mL	4.0213 mL
	20 mM	0.1206 mL	0.6032 mL	1.2064 mL	3.0160 mL

Bioz

Keywords

Momelotinib

19 Cited Publications

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Momelotinib

Publications Citing Use of MedChemExpress (MCE) Momelotinib

All JAK Isoforms