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Version: 17.06d (Release date: 2017-06-26)
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Ralimetinib Mesylate (Code C105853)

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Terms & Properties

Preferred Name: Ralimetinib Mesylate

Definition: The dimesylate salt form of LY2228820, a tri-substituted imidazole derivative and orally available, p38 mitogen-activated protein kinase (MAPK) inhibitor with potential anti-inflammatory and antineoplastic activities. Upon administration, ralimetinib inhibits the activity of p38, particularly the alpha and beta isoforms, thereby inhibiting MAPKAPK2 phosphorylation and preventing p38 MAPK-mediated signaling. This may inhibit the production of a variety of cytokines involved in inflammation, cellular proliferation and angiogenesis such as tumor necrosis factor alpha (TNFa), interleukin (IL)-1, -6 and -8, vascular endothelial growth factor, and macrophage inflammatory protein-1 alpha. Ultimately this induces apoptosis and reduces tumor cell proliferation. In addition, inhibition of the p38 MAPK pathway by LY2228820 increases the antineoplastic activity of certain chemotherapeutic agents. p38 MAPK, a serine/threonine protein kinase that is often upregulated in cancer cells, plays a crucial role in tumor cell proliferation, angiogenesis and metastasis.

Display Name: Ralimetinib Mesylate

Label: Ralimetinib Mesylate

NCI Thesaurus Code: C105853 (Search for linked caDSR metadata)  (search value sets)

NCI Metathesaurus Link: C3661088  (see NCI Metathesaurus info)

Synonyms & Abbreviations: (see Synonym Details)
3H-Imidazo(4,5-b)pyridin-2-amine, 5-(2-(1,1-dimethylethyl)-4-(4-fluorophenyl)-1H-imidazol-5-yl)-3-(2,2-dimethylpropyl)-, Methanesulfonate (1:2)
LY-2228820
LY2228820
LY2228820 Dimesylate
Ralimetinib Dimesylate
Ralimetinib Mesylate
RALIMETINIB MESYLATE

External Source Codes: 
CAS Registry Number 862507-23-1 (see NLM ChemIDplus info)
FDA UNII Code QUW7B71FO9
PDQ Closed Trial Search ID 687387
PDQ Open Trial Search ID 687387 (check for NCI PDQ open clinical trial info)
UMLS CUI C3661088

Other Properties:
     Name Value (qualifiers indented underneath)
code C105853
Contributing_Source CTRP
Contributing_Source FDA
Semantic_Type Pharmacologic Substance

Additional Concept Data: 
Defined Fully by Roles: No  

URL: https://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C105853

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