Preferred Label : Ralimetinib;
NCIt synonyms : 3H-Imidazo(4,5-b)pyridin-2-amine, 5-(2-(1,1-Dimethylethyl)-4-(4-fluorophenyl)-1H-imidazol-5-yl)-3-(2,2-dimethylpropyl)-; LY2228820 Free Base;
NCIt definition : 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 ralimetinib 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 : 73I34XW4HD;
InChIKey : XPPBBJCBDOEXDN-UHFFFAOYSA-N;
CAS number : 862505-00-8;
NCI Metathesaurus CUI : CL541474;
Origin ID : C143046;
UMLS CUI : C4519218;
Currated CISMeF NLP mapping
- Semantic type(s)
- UMLS correspondences (same concept)
- concept_is_in_subset
- has_salt_form
- is_free_acid_or_base_form_of
