Preferred Label : Ralimetinib Mesylate;
NCIt synonyms : Ralimetinib Dimesylate; LY2228820 Dimesylate; 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);
NCIt 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.;
UNII : QUW7B71FO9;
InChIKey : NARMJPIBAXVUIE-UHFFFAOYSA-N;
CAS number : 862507-23-1;
Molecule name : LY-2228820;
Origin ID : C105853;
UMLS CUI : C4331816;
Automatic exact mappings (from CISMeF team)
- Semantic type(s)
- concept_is_in_subset
- has_free_acid_or_base_form
- has_target
- is_salt_form_of
