" /> Belumosudil Mesylate - CISMeF





Preferred Label : Belumosudil Mesylate;

NCIt synonyms : KD025 Mesylate; 2-(3-(4-(1H-indazol-5-ylamino)quinazolin-2-yl)phenoxy)-N-(propan-2-yl)acetamide Methanesulfonate (1:1); Acetamide, 2-(3-(4-(1H-indazol-5-ylamino)-2-quinazolinyl)phenoxy)-N-(1-methylethyl)-, Methanesulfonate (1:1);

NCIt definition : The mesylate salt form of belumosudil, an orally bioavailable inhibitor of Rho-associated coiled-coil kinase 2 (ROCK2; ROCK-II), with potential immunomodulating activity. Upon oral administration, belumosudil binds to and inhibits the serine/threonine kinase activity of ROCK2. This inhibits ROCK2-mediated signal transduction pathways and modulates various pro- and anti-inflammatory immune cell responses through the regulation of signal transducer and activator of transcription 3 and 5 (STAT3/STAT5) phosphorylation. This downregulates pro-inflammatory Th17 cells and increases regulatory T (Treg) cells. Belumosudil also inhibits ROCK2-mediated fibrotic processes, including stress fiber formation, myofibroblast activation and pro-fibrotic gene transcription. ROCK2 is upregulated in various diseases, including various fibrotic, neurodegenerative and autoimmune diseases.;

UNII : 6MX7XE1M0U;

InChIKey : ILQJXEIRBCHLOM-UHFFFAOYSA-N;

CAS number : 2109704-99-4;

Drug name : Rezurock;

NCI Metathesaurus CUI : CL1412310;

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30/05/2025


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