Home Cart Sign in  
Chemical Structure| 1056634-68-4 Chemical Structure| 1056634-68-4

Structure of Momelotinib
CAS No.: 1056634-68-4

Chemical Structure| 1056634-68-4

*Storage: {[sel_prStorage]}

*Shipping: {[sel_prShipping]}

,{[proInfo.pro_purity]}

Momelotinib (CYT387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 values of 11 nM and 18 nM, respectively, showing significantly less activity against JAK3.

Synonyms: CYT387; LM-1149; CYT11387

4.5 *For Research Use Only !

{[proInfo.pro_purity]}
Cat. No.: {[proInfo.prAm]} Purity: {[proInfo.pro_purity]}

Change View

Size Price VIP Price

US Stock

Global Stock

In Stock
{[ item.pr_size ]} Inquiry {[ getRatePrice(item.pr_usd,item.pr_rate,item.mem_rate,item.pr_is_large_size_no_price, item.vip_usd) ]}

US Stock: ship in 0-1 business day
Global Stock: ship in 5-7 days

  • {[ item.pr_size ]}

In Stock

- +

Please Login or Create an Account to: See VIP prices and availability

US Stock: ship in 0-1 business day
Global Stock: ship in 2 weeks

  • 1-2 Day Shipping
  • High Quality
  • Technical Support
Product Citations

Alternative Products

Product Details of Momelotinib

CAS No. :1056634-68-4
Formula : C23H22N6O2
M.W : 414.46
SMILES Code : O=C(NCC#N)C1=CC=C(C=C1)C1=CC=NC(NC2=CC=C(C=C2)N2CCOCC2)=N1
Synonyms :
CYT387; LM-1149; CYT11387
MDL No. :MFCD16038899
InChI Key :ZVHNDZWQTBEVRY-UHFFFAOYSA-N
Pubchem ID :25062766

Safety of Momelotinib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of Momelotinib

epigenetics
RTK
JAK-STAT

Isoform Comparison

Biological Activity

Target
  • JAK1

    JAK1, IC50:11 nM

  • JAK3

    JAK3, IC50:155 nM

  • JAK2

    JAK2, IC50:18 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
CBL-mutant iPSC-derived myeloid cells 1 uM 60 minutes Inhibited JAK/STAT signaling, significantly decreased pJAK2 and pSTAT5 levels PMC6286697
HHSteCs 2 µM 24 hours Momelotinib attenuated the phosphorylation of STAT1 and reduced COL1A1 production. PMC8251927
Colon cancer cells 1 nM to 1 μM 96 hours To evaluate the inhibitory effect of Momelotinib on the proliferation of colon cancer cells, the results showed that Momelotinib significantly inhibited cell proliferation PMC6343337
8988T cells 5 μM 60 minutes inhibits autophagy and reduces PD-L1 expression PMC4891226
8988T-LC3-GFP cells 5 μM 60 minutes inhibits autophagy PMC4891226
U937-derived macrophages 25 ng/mL 72 hours IL-11 enhances pro-tumoral features of macrophages via the AXL-STAT3 signaling pathway, upregulating CD44 expression. PMC10577802
AML cell lines 2.5 µM 6 hours To evaluate the effect of Momelotinib on AML cell lines, results showed that Momelotinib inhibited MYC mRNA and protein expression. PMC6290107
MOLM14 cells 0.625 µM 2 hours To evaluate the effect of Momelotinib on MOLM14 cells, results showed that Momelotinib significantly reduced YB-1 phosphorylation. PMC6290107
BaF3 cells 325 nM 72 hours Momelotinib effectively suppressed the proliferation of BaF3-JAK2V617F cells with an IC50 of 325 nM. PMC8864657
MV4-11 cells 165 nM 2 hours Momelotinib significantly inhibited pFLT3 and pSTAT5 levels in MV4-11 cells within 2 hours, with an IC50 of 165 nM. PMC8864657

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
mice cerulein-induced pancreatitis model oral 100 mg/kg Once every 5 days for 4 weeks inhibits autophagy and reduces inflammation PMC4891226
Nu/J mice A549 lung cancer xenograft model Oral 50 mg/kg daily for 2 days Momelotinib inhibits JAK1/2 signaling, reducing recruitment of tumor-associated macrophages and suppressing tumor growth. PMC10577802
NSG mice human AML xenograft model oral 10 mg/kg once daily for 30 days To evaluate the therapeutic effect of Momelotinib in the AML xenograft model, results showed that Momelotinib significantly reduced tumor burden and decreased IKBKE, YB-1 phosphorylation, and MYC expression. PMC6290107
Mice NSGS mice Intraperitoneal injection 10 mg/kg daily for 10 days Momelotinib effectively suppressed leukemic progression in the NSGS mouse model, whereas gilteritinib treatment was ineffective. PMC8864657

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT02251821 Primary Myelofibrosis ... More >> Secondary Myelofibrosis Less << Phase 2 Recruiting - United States, Washington ... More >> Fred Hutch/University of Washington Cancer Consortium Recruiting Seattle, Washington, United States, 98109 Contact: Rachel B. Salit    206-667-1317    rsalit@fredhutch.org    Principal Investigator: Rachel B. Salit Less <<
NCT02206763 EGFR Mutated EGFR TKI Naive Me... More >>tastatic NSCLC Less << Phase 1 Terminated - United States, California ... More >> Duarte, California, United States Palo Alto, California, United States Whittier, California, United States Less <<
NCT01998828 Polycythemia Vera|Essential Th... More >>rombocythemia Less << PHASE2 TERMINATED 2015-05-07 Scottsdale, Arizona, United St... More >>ates|Whittier, California, United States|Tupelo, Mississippi, United States|Saint Louis, Missouri, United States|Houston, Texas, United States|Frankston, Victoria, Australia|Parkville, Victoria, Australia|Vancouver, British Columbia, Canada|Toronto, Ontario, Canada|Montreal, Quebec, Canada|La Tronche, France|Nantes Cedex 1, France|Paris, France|Dresden, Germany|Minden, Germany Less <<
NCT01969838 Primary Myelofibrosis ... More >> Post-Polycythemia Vera Myelofibrosis Post-Essential Thrombocythemia Myelofibrosis Less << Phase 3 Active, not recruiting March 2019 -
NCT02101021 Metastatic Pancreatic Ductal A... More >>denocarcinoma Less << Phase 3 Terminated - United States, California ... More >> Cedars-Sinai Medical Center Los Angeles, California, United States, 90048 United States, Indiana Indiana University Health Goshen Center for Cancer Care Goshen, Indiana, United States, 46506 United States, Massachusetts Dana Farber Cancer Institute Boston, Massachusetts, United States, 02215 United States, Washington Northwest Medical Specialties, PLLC Tacoma, Washington, United States, 98405 Less <<
NCT02101268 Primary Myelofibrosis (PMF) ... More >> Post-polycythemia Vera (Post-PV) Post-essential Thrombocythemia Myelofibrosis (Post-ET MF) Less << Phase 3 Active, not recruiting March 2019 -
NCT02101021 - Terminated - -
NCT02515630 Primary Myelofibrosis (PMF) ... More >> Post-polycythemia Vera (Post-PV) Myelofibrosis Postessential Thrombocythemia (Post-ET) Myelofibrosis Less << Phase 2 Completed - United States, Arizona ... More >> Phoenix, Arizona, United States United States, California Los Angeles, California, United States Orange, California, United States United States, Florida Jacksonville, Florida, United States United States, Maryland Baltimore, Maryland, United States United States, Michigan Ann Arbor, Michigan, United States United States, Missouri Saint Louis, Missouri, United States United States, New York Bronx, New York, United States New York, New York, United States United States, North Carolina Durham, North Carolina, United States United States, Ohio Cleveland, Ohio, United States United States, Texas Houston, Texas, United States Canada, Ontario Toronto, Ontario, Canada Less <<
NCT02258607 Relapsed Metastatic KRAS-Mutat... More >>ed Non-Small Cell Lung Cancer Less << Phase 1 Terminated - United States, California ... More >> Duarte, California, United States Sacramento, California, United States United States, Massachusetts Boston, Massachusetts, United States United States, Virginia Fairfax, Virginia, United States United States, Washington Spokane, Washington, United States Less <<
NCT01423058 Primary Myelofibrosis|Post-Pol... More >>ycythemia Vera|Post-Essential Thrombocythemia Myelofibrosis Less << PHASE1|PHASE2 COMPLETED 2025-06-14 Mayo Clinic, Scottsdale, Arizo... More >>na, 85259, United States|Mayo Clinic, Jacksonville, Florida, 32224, United States|MD Anderson Cancer Center, The University of Texas, Houston, Texas, 77030, United States|Huntsman Cancer Institute at the University of Utah, Salt Lake City, Utah, 84108, United States|Princess Margaret Hospital, Toronto, Ontario, M5G 2M9, Canada|Jewish General Hospital, Montreal, Quebec, H3T 1E2, Canada Less <<
NCT01236638 Primary Myelofibrosis|Post-Pol... More >>ycythemia Vera Myelofibrosis|Post-Essential Thrombocythemia Myelofibrosis Less << PHASE2 COMPLETED 2025-06-14 Stanford Cancer Center, Stanfo... More >>rd, California, 94305-5821, United States|Dana-Farber Cancer Institute, Boston, Massachusetts, 02115, United States|Mayo Clinic, Rochester, Minnesota, 55905, United States|The Royal Melbourne Hospital, Parkville, Victoria, 3050, Australia|Princess Margaret Hospital, Toronto, Ontario, M5G 2M9, Canada|Jewish General Hospital, Montreal, Quebec, H3T 1E2, Canada Less <<
NCT02124746 Primary Myelofibrosis|Post-Pol... More >>ycythemia Vera Myelofibrosis|Post-Essential Thrombocythemia Myelofibrosis|Polycythemia Vera|Essential Thrombocythemia Less << PHASE2 COMPLETED 2018-12-06 Scottsdale, Arizona, United St... More >>ates|Orange, California, United States|Stanford, California, United States|Whittier, California, United States|Jacksonville, Florida, United States|Baltimore, Maryland, United States|Boston, Massachusetts, United States|Ann Arbor, Michigan, United States|Rochester, Minnesota, United States|Saint Louis, Missouri, United States|Bronx, New York, United States|New York, New York, United States|Cleveland, Ohio, United States|Houston, Texas, United States|Salt Lake City, Utah, United States|Frankston, Victoria, Australia|Parkville, Victoria, Australia|Toronto, Ontario, Canada|Montreal, Quebec, Canada|La Tronche, France|Paris, France|Minden, Germany Less <<
NCT02244489 Relapsed/Refractory Metastatic... More >> Pancreatic Ductal Adenocarcinoma Less << Phase 1 Terminated - United States, Arizona ... More >> Scottsdale Healthcare Research Institute Scottsdale, Arizona, United States, 85258 United States, California Cedars-Sinai Medical Center Los Angeles, California, United States, 90048 United States, Tennessee Tennessee Oncology Nashville, Tennessee, United States, 37203 United States, Virginia Virginia Cancer Specialists, PC Fairfax, Virginia, United States, 22031 Less <<
NCT03441113 Post-polycythemia Vera Myelofi... More >>brosis (Post-PV MF) Primary Myelofibrosis (PMF) Post-essential Thrombocythemia Myelofibrosis (Post-ET MF) Less << Phase 2 Enrolling by invitation June 2020 -
NCT00935987 Primary Myelofibrosis|Post-Pol... More >>ycythemia Vera Myelofibrosis|Post-Essential Thrombocythemia Myelofibrosis Less << PHASE1|PHASE2 COMPLETED 2025-04-12 Stanford Cancer Center, Stanfo... More >>rd, California, 94305-5821, United States|Dana-Farber Cancer Institute, Boston, Massachusetts, 02115, United States|Mayo Clinic, Rochester, Minnesota, 55905, United States|The Royal Melbourne Hospital, Parkville, Victoria, 3050, Australia|Princess Margaret Hospital, Toronto, Ontario, M5G 2M9, Canada|Jewish General Hospital, Montreal, Quebec, H3T 1E2, Canada Less <<
NCT05582083 Myelofibrosis|Primary Myelofib... More >>rosis Less << NO_LONGER_AVAILABLE - -

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.41mL

0.48mL

0.24mL

12.06mL

2.41mL

1.21mL

24.13mL

4.83mL

2.41mL

 

Historical Records

Categories