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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)
LY2228820 Dimesylate
Ralimetinib Dimesylate
Ralimetinib Mesylate

External Source Codes: 
CAS Registry Number 862507-23-1 (see NLM ChemIDplus info)
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  


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