Momelotinib (CYT387)

Name Value
Weight 414.469 g/mol
Zinc ID ZINC43199890
Smiles C1COCCN1C2=CC=C(C=C2)NC3=NC=CC(=N3)C4=CC=C(C=C4)C(=O)NCC#N
Molecular formula C23H22N6O2
Mode of inhibition ATP competitive JAK1 and JAK2 inhibitor, STAT indirect inhibitor; Tyrosine kinase inhibitors
CAS 1056634-68-4

Clinical Trials

Study title Status Conditions Link
Safety and Efficacy Study of CYT387 in Primary Myelofibrosis (PMF) or Post-polycythemia Vera (PV) or Post-essential Thrombocythemia (ET) Completed Primary Myelofibrosis|Post-Polycythemia Vera Myelofibrosis|Post-Essential Thrombocythemia Myelofibrosis NCT00935987
Extension Study Evaluating the Long Term Safety and Efficacy Study of CYT387 in Primary Myelofibrosis (PMF) or Post-polycythemia Vera (PV) or Post-essential Thrombocythemia (ET) Completed Primary Myelofibrosis|Post-Polycythemia Vera Myelofibrosis|Post-Essential Thrombocythemia Myelofibrosis NCT01236638
Safety Study Evaluating Twice-Daily Administration of Momelotinib in Primary Myelofibrosis or Post-Polycythemia Vera or Post-Essential Thrombocythemia Myelofibrosis Completed Primary Myelofibrosis|Post-Polycythemia Vera|Post-Essential Thrombocythemia Myelofibrosis NCT01423058
Extended Access of Momelotinib in Adults With Myelofibrosis Enrolling by invitation Post-polycythemia Vera Myelofibrosis (Post-PV MF)|Primary Myelofibrosis (PMF)|Post-essential Thrombocythemia Myelofibrosis (Post-ET MF) NCT03441113
Momelotinib in Transfusion-Dependent Adults With Primary Myelofibrosis (PMF) or Post-polycythemia Vera or Post-essential Thrombocythemia Myelofibrosis (Post-PV/ET MF) Completed Primary Myelofibrosis (PMF)|Post-polycythemia Vera (Post-PV) Myelofibrosis|Postessential Thrombocythemia (Post-ET) Myelofibrosis NCT02515630
Efficacy and Safety of Momelotinib Combined With Trametinib in Adults With Metastatic KRAS-mutated Non-Small Cell Lung Cancer (NSCLC) Who Have Failed Platinum-Based Chemotherapy Preceded by a Dose-finding Lead-in Phase Terminated Relapsed Metastatic KRAS-Mutated Non-Small Cell Lung Cancer NCT02258607
Momelotinib Combined With Capecitabine and Oxaliplatin in Adults With Relapsed/Refractory Metastatic Pancreatic Ductal Adenocarcinoma Terminated Relapsed/Refractory Metastatic Pancreatic Ductal Adenocarcinoma NCT02244489
Long-term Safety and Efficacy of Momelotinib in Subjects With Primary Myelofibrosis, Post-polycythemia Vera Myelofibrosis, Post-essential Thrombocythemia Myelofibrosis, Polycythemia Vera or Essential Thrombocythemia Completed Primary Myelofibrosis|Post-Polycythemia Vera Myelofibrosis|Post-Essential Thrombocythemia Myelofibrosis|Polycythemia Vera|Essential Thrombocythemia NCT02124746
Efficacy of Momelotinib Versus Best Available Therapy in Anemic or Thrombocytopenic Subjects With Primary Myelofibrosis (MF), Post-polycythemia Vera MF, or Post-essential Thrombocythemia MF Active, not recruiting Primary Myelofibrosis (PMF)|Post-polycythemia Vera (Post-PV)|Post-essential Thrombocythemia Myelofibrosis (Post-ET MF) NCT02101268
Gemcitabine and Nab-paclitaxel Combined With Momelotinib in Participants With Previously Untreated Metastatic Pancreatic Ductal Adenocarcinoma Terminated Metastatic Pancreatic Ductal Adenocarcinoma NCT02101021
Safety and Efficacy of Momelotinib in Subjects With Polycythemia Vera or Essential Thrombocythemia Terminated Polycythemia Vera|Essential Thrombocythemia NCT01998828
Momelotinib Versus Ruxolitinib in Subjects With Myelofibrosis Active, not recruiting Primary Myelofibrosis|Post-Polycythemia Vera Myelofibrosis|Post-Essential Thrombocythemia Myelofibrosis NCT01969838
A Study of Momelotinib Versus Danazol in Symptomatic and Anemic Myelofibrosis Patients (MOMENTUM) Recruiting Primary Myelofibrosis|Post-polycythemia Vera Myelofibrosis|Post-essential Thrombocythemia Myelofibrosis NCT04173494
Erlotinib and Momelotinib for the Treatment of Epidermal Growth Factor Receptor (EGFR) Mutated EGFR Tyrosine Kinase Inhibitor (TKI) Naive Metastatic Non-Small Cell Lung Cancer (NSCLC) Terminated EGFR Mutated EGFR TKI Naive Metastatic NSCLC NCT02206763

References

Publication DOI Pubmed PMCID
Posterior subcapsular cataracts. Related to long-term corticosteroid treatment in children. American journal of diseases of children (1960) M Bihari, B J Grossman, 116, 6, None, None, 10.1111/jvim.14837 10.1111/jvim.14837 5697192 28960447
Inhibition of JAK/STAT pathway restrains TSLP-activated dendritic cells mediated inflammatory T helper type 2 cell response in allergic rhinitis. Molecular and cellular biochemistry Zhaohui Shi, Weihong Jiang, Min Wang, Xiaocheng Wang, Xiaoyuan Li, Xiaodong Chen, Li Qiao, 430, 1-2, None, 2017-02-18, 10.1007/s11010-017-2963-7 10.1007/s11010-017-2963-7 28214951 28214951

Vendors

Company Lnk to product
MedChemExpress https://www.medchemexpress.com/CYT387.html
Selleckchem https://www.selleckchem.com/products/Cyt387.html
Adooq Bioscience https://www.adooq.com/cyt387.html

Filter data

Compound Momelotinib (CYT387)
Experiment types CellTiter96 AQueous One Solution Cell Proliferation assays, ELISA, ELISPOT, Flow cytometry , Histopathological staining , Ki67/DAPI cell proliferation assay, MFI, MTS, RT-PCR, RT-qPCR, Trypan blue exclusion assay, Western Blot
Concentrations 1.00, 1.50, 100.00, 2.00, 3.00, 30.00, 4.00, 5.00, 6.00, 8.00, N/A
Cell lines CLBL-1, DC, DLBCL primary cells, MDCK, OLC-LY7, nasal mucosa
Organisms Canis familriaris, Homo sapiens, Mus musculus
Animal models AR, patient 1, patient 2, patient 3
STAT proteins STAT1, STAT3, STAT5, p-STAT1, p-STAT3, p-STAT5
Other CD11c, CD80, CD86, GAPDH, IFNγ, IL-4, IL-5, JAK1, JAK2, MHC class II, OX-40L, p-JAK1, p-JAK2, β-actin

Experiments

Compound Experiment type Investigated event Concentration Cell line Organism Animal model Stat protein Details
Momelotinib (CYT387) Trypan blue exclusion assay Influence on cell growth 1.00 µM MDCK Canis familriaris
Momelotinib (CYT387) Trypan blue exclusion assay Influence on cell growth 1.00 µM CLBL-1 Canis familriaris
Momelotinib (CYT387) Trypan blue exclusion assay Influence on cell growth 2.00 µM MDCK Canis familriaris
Momelotinib (CYT387) Trypan blue exclusion assay Influence on cell growth 2.00 µM CLBL-1 Canis familriaris
Momelotinib (CYT387) Trypan blue exclusion assay Influence on cell growth 5.00 µM MDCK Canis familriaris
Momelotinib (CYT387) Trypan blue exclusion assay Influence on cell growth 5.00 µM CLBL-1 Canis familriaris
Momelotinib (CYT387) MTS Influence on cell growth 1.00 µM MDCK Canis familriaris
Momelotinib (CYT387) MTS Influence on cell growth 2.00 µM MDCK Canis familriaris
Momelotinib (CYT387) MTS Influence on cell growth 5.00 µM MDCK Canis familriaris
Momelotinib (CYT387) MTS Influence on cell growth 1.00 µM CLBL-1 Canis familriaris
Momelotinib (CYT387) MTS Influence on cell growth 2.00 µM CLBL-1 Canis familriaris
Momelotinib (CYT387) MTS Influence on cell growth 5.00 µM CLBL-1 Canis familriaris
Momelotinib (CYT387) CellTiter96 AQueous One Solution Cell Proliferation assays Influence on cell proliferation 1.00 µM CLBL-1 Canis familriaris
Momelotinib (CYT387) CellTiter96 AQueous One Solution Cell Proliferation assays Influence on cell proliferation 2.00 µM CLBL-1 Canis familriaris
Momelotinib (CYT387) CellTiter96 AQueous One Solution Cell Proliferation assays Influence on cell proliferation 5.00 µM CLBL-1 Canis familriaris
Momelotinib (CYT387) MTS Influence on cell proliferation 2.00 µM CLBL-1 Canis familriaris
Momelotinib (CYT387) MTS Influence on cell proliferation 4.00 µM CLBL-1 Canis familriaris
Momelotinib (CYT387) MTS Influence on cell proliferation 6.00 µM CLBL-1 Canis familriaris
Momelotinib (CYT387) MTS Influence on cell proliferation 8.00 µM CLBL-1 Canis familriaris
Momelotinib (CYT387) MTS Influence on cell proliferation 1.00 µM DLBCL primary cells Canis familriaris patient 1
Momelotinib (CYT387) MTS Influence on cell proliferation 2.00 µM DLBCL primary cells Canis familriaris patient 1
Momelotinib (CYT387) MTS Influence on cell proliferation 3.00 µM DLBCL primary cells Canis familriaris patient 1
Momelotinib (CYT387) MTS Influence on cell proliferation 4.00 µM DLBCL primary cells Canis familriaris patient 1
Momelotinib (CYT387) MTS Influence on cell proliferation 5.00 µM DLBCL primary cells Canis familriaris patient 1
Momelotinib (CYT387) MTS Influence on cell proliferation 1.00 µM DLBCL primary cells Canis familriaris patient 2
Momelotinib (CYT387) MTS Influence on cell proliferation 2.00 µM DLBCL primary cells Canis familriaris patient 2
Momelotinib (CYT387) MTS Influence on cell proliferation 3.00 µM DLBCL primary cells Canis familriaris patient 2
Momelotinib (CYT387) MTS Influence on cell proliferation 4.00 µM DLBCL primary cells Canis familriaris patient 2
Momelotinib (CYT387) MTS Influence on cell proliferation 5.00 µM DLBCL primary cells Canis familriaris patient 2
Momelotinib (CYT387) MTS Influence on cell proliferation 1.00 µM DLBCL primary cells Canis familriaris patient 3
Momelotinib (CYT387) MTS Influence on cell proliferation 2.00 µM DLBCL primary cells Canis familriaris patient 3
Momelotinib (CYT387) MTS Influence on cell proliferation 3.00 µM DLBCL primary cells Canis familriaris patient 3
Momelotinib (CYT387) MTS Influence on cell proliferation 4.00 µM DLBCL primary cells Canis familriaris patient 3
Momelotinib (CYT387) MTS Influence on cell proliferation 5.00 µM DLBCL primary cells Canis familriaris patient 3
Momelotinib (CYT387) MTS Influence on cell proliferation 1.00 µM OLC-LY7 Homo sapiens
Momelotinib (CYT387) MTS Influence on cell proliferation 2.00 µM OLC-LY7 Homo sapiens
Momelotinib (CYT387) MTS Influence on cell proliferation 3.00 µM OLC-LY7 Homo sapiens
Momelotinib (CYT387) MTS Influence on cell proliferation 4.00 µM OLC-LY7 Homo sapiens
Momelotinib (CYT387) MTS Influence on cell proliferation 5.00 µM OLC-LY7 Homo sapiens
Momelotinib (CYT387) RT-qPCR Influence on RNA expression N/A µM CLBL-1 Canis familriaris
Momelotinib (CYT387) RT-qPCR Influence on RNA expression N/A µM CLBL-1 Canis familriaris
Momelotinib (CYT387) Western Blot Influence on protein activity 1.00 µM CLBL-1 Canis familriaris
Momelotinib (CYT387) Western Blot Influence on protein activity 2.00 µM CLBL-1 Canis familriaris
Momelotinib (CYT387) Western Blot Influence on protein activity 5.00 µM CLBL-1 Canis familriaris
Momelotinib (CYT387) Western Blot Influence on protein activity 1.00 µM CLBL-1 Canis familriaris p-STAT3
Momelotinib (CYT387) Western Blot Influence on protein activity 2.00 µM CLBL-1 Canis familriaris p-STAT3
Momelotinib (CYT387) Western Blot Influence on protein activity 5.00 µM CLBL-1 Canis familriaris p-STAT3
Momelotinib (CYT387) Western Blot Influence on protein activity 1.00 µM CLBL-1 Canis familriaris
Momelotinib (CYT387) Western Blot Influence on protein activity 2.00 µM CLBL-1 Canis familriaris
Momelotinib (CYT387) Western Blot Influence on protein activity 5.00 µM CLBL-1 Canis familriaris
Momelotinib (CYT387) Flow cytometry Influence on STAT3 activity in presence of IL6 1.50 µM CLBL-1 Canis familriaris p-STAT3
Momelotinib (CYT387) MFI Influence on STAT3 activity in presence of IL6 1.50 µM CLBL-1 Canis familriaris p-STAT3
Momelotinib (CYT387) Flow cytometry Influence on cell apoptosis 1.00 µM CLBL-1 Canis familriaris
Momelotinib (CYT387) Flow cytometry Influence on cell apoptosis 5.00 µM CLBL-1 Canis familriaris
Momelotinib (CYT387) Flow cytometry Influence on cell apoptosis 1.00 µM MDCK Canis familriaris
Momelotinib (CYT387) Flow cytometry Influence on cell apoptosis 5.00 µM MDCK Canis familriaris
Momelotinib (CYT387) Ki67/DAPI cell proliferation assay Influence on cell cycle 1.00 µM CLBL-1 Canis familriaris
Momelotinib (CYT387) Western Blot Influence on protein activity in response to TSLP stimulation 100.00 nM DC Mus musculus
Momelotinib (CYT387) Western Blot Influence on protein activity in response to TSLP stimulation 100.00 nM DC Mus musculus
Momelotinib (CYT387) Western Blot Influence on protein activity in response to TSLP stimulation 100.00 nM DC Mus musculus
Momelotinib (CYT387) Western Blot Influence on protein activity in response to TSLP stimulation 100.00 nM DC Mus musculus
Momelotinib (CYT387) Western Blot Influence on protein activity in response to TSLP stimulation 100.00 nM DC Mus musculus p-STAT1
Momelotinib (CYT387) Western Blot Influence on protein activity in response to TSLP stimulation 100.00 nM DC Mus musculus STAT1
Momelotinib (CYT387) Western Blot Influence on protein activity in response to TSLP stimulation 100.00 nM DC Mus musculus p-STAT3
Momelotinib (CYT387) Western Blot Influence on protein activity in response to TSLP stimulation 100.00 nM DC Mus musculus STAT3
Momelotinib (CYT387) Western Blot Influence on protein activity in response to TSLP stimulation 100.00 nM DC Mus musculus p-STAT5
Momelotinib (CYT387) Western Blot Influence on protein activity in response to TSLP stimulation 100.00 nM DC Mus musculus STAT5
Momelotinib (CYT387) Flow cytometry Influence on surface protein 100.00 nM DC Mus musculus
Momelotinib (CYT387) Flow cytometry Influence on surface protein 100.00 nM DC Mus musculus
Momelotinib (CYT387) Flow cytometry Influence on surface protein 100.00 nM DC Mus musculus
Momelotinib (CYT387) Flow cytometry Influence on surface protein 100.00 nM DC Mus musculus
Momelotinib (CYT387) Western Blot Influence on surface protein 100.00 nM DC Mus musculus
Momelotinib (CYT387) RT-PCR Influence on surface protein 100.00 nM DC Mus musculus
Momelotinib (CYT387) Flow cytometry Influence on inflammatory Th2 cell response 100.00 nM DC Mus musculus
Momelotinib (CYT387) ELISA Influence on cytokine levels 100.00 nM DC Mus musculus
Momelotinib (CYT387) ELISA Influence on cytokine levels 100.00 nM DC Mus musculus
Momelotinib (CYT387) ELISA Influence on cytokine levels 100.00 nM DC Mus musculus
Momelotinib (CYT387) Histopathological staining Influence on Th2 response 30.00 mg/kg nasal mucosa Mus musculus AR
Momelotinib (CYT387) Western Blot Influence on Th2 response 30.00 mg/kg nasal mucosa Mus musculus AR
Momelotinib (CYT387) Western Blot Influence on Th2 response 30.00 mg/kg nasal mucosa Mus musculus AR
Momelotinib (CYT387) ELISA Influence on cytokine levels 30.00 mg/kg nasal mucosa Mus musculus AR
Momelotinib (CYT387) ELISA Influence on cytokine levels 30.00 mg/kg nasal mucosa Mus musculus AR
Momelotinib (CYT387) ELISA Influence on cytokine levels 30.00 mg/kg nasal mucosa Mus musculus AR
Momelotinib (CYT387) ELISPOT Influence on cytokine levels 30.00 mg/kg nasal mucosa Mus musculus AR
Momelotinib (CYT387) ELISPOT Influence on cytokine levels 30.00 mg/kg nasal mucosa Mus musculus AR