Momelotinib (INN, formerly GS-0387, CYT-387) is an inhibitor of Janus kinases JAK1 and JAK2, acting as an ATP competitor with IC50 values of 11 and 18 nM, respectively. The inhibitor is significantly less active towards other kinases, including JAK3 (IC50 = 0.16 μM). As of 2011, momelotinib is being developed as a drug for myelofibrosis and currently undergoes Phase I/II clinical trials. Additional potential treatment indications for momelotinib include other myeloproliferative neoplasms, cancer (solid and liquid tumors) and inflammatory conditions.
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| dbo:abstract |
Momelotinib (INN, formerly GS-0387, CYT-387) is an inhibitor of Janus kinases JAK1 and JAK2, acting as an ATP competitor with IC50 values of 11 and 18 nM, respectively. The inhibitor is significantly less active towards other kinases, including JAK3 (IC50 = 0.16 μM). As of 2011, momelotinib is being developed as a drug for myelofibrosis and currently undergoes Phase I/II clinical trials. Additional potential treatment indications for momelotinib include other myeloproliferative neoplasms, cancer (solid and liquid tumors) and inflammatory conditions. As of 2016, momelotinib is being investigated for primary myelofibrosis or post-polycythemia vera or post-essential thrombocythemia myelofibrosis (post-PV/ET MF), as well as a treatment for relapsed or refractory metastatic pancreatic ductal adenocarcinoma (in combination with capecitabine and oxaliplatin). (en) |
| dbo:alternativeName |
CYT-387, CYT-11387, GS-0387 (en) |
| dbo:iupacName |
N-(Cyanomethyl)-4-{2-[4-(morpholin-4-yl)anilino]pyrimidin-4-yl}benzamide (en) |
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wiki-commons:Special:FilePath/Momelotinib.svg?width=300 |
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https://oncologytube.com/video/41076/momelotinib-a-jak-inhibitor-vs-danazol-in-myelofibrosis%3FchannelName=EHA https://web.archive.org/web/20100506060243/http:/www.ymbiosciences.com/patients/cyt387.php |
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Momelotinib.svg (en) |
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255 (xsd:integer) |
| dbp:othernames |
CYT-387, CYT-11387, GS-0387 (en) |
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N--4-{2-[4-anilino]pyrimidin-4-yl}benzamide (en) |
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dbc:Experimental_cancer_drugs dbc:Benzamides dbc:Aminopyrimidines dbc:Morpholines dbc:Nitriles dbc:Protein_kinase_inhibitors dbc:Non-receptor_tyrosine_kinase_inhibitors |
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owl:Thing dul:ChemicalObject dbo:ChemicalSubstance wikidata:Q11173 dbo:ChemicalCompound |
| rdfs:comment |
Momelotinib (INN, formerly GS-0387, CYT-387) is an inhibitor of Janus kinases JAK1 and JAK2, acting as an ATP competitor with IC50 values of 11 and 18 nM, respectively. The inhibitor is significantly less active towards other kinases, including JAK3 (IC50 = 0.16 μM). As of 2011, momelotinib is being developed as a drug for myelofibrosis and currently undergoes Phase I/II clinical trials. Additional potential treatment indications for momelotinib include other myeloproliferative neoplasms, cancer (solid and liquid tumors) and inflammatory conditions. (en) |
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Momelotinib (en) |
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