Structure of Momelotinib
CAS No.: 1056634-68-4
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
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
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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 |
GHS Pictogram: |
![]() |
Signal Word: | Warning |
Hazard Statements: | H302 |
Precautionary Statements: | P280-P305+P351+P338 |
Target |
|
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 | - | - |
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 |
Tags: Momelotinib | CYT387 | CYT 387 | CYT-387 | JAK | Autophagy | Apoptosis | Janus kinase | 1056634-68-4
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