Preferred Label : Soquelitinib;
NCIt synonyms : Interleukin-2 Inducible T-cell Kinase Inhibitor CPI-818; ITK Inhibitor CPI-818;
NCIt definition : An orally available, small-molecule, irreversible inhibitor of interleukin-2 inducible
T-cell kinase (ITK) with potential immunomodulatory and antineoplastic activities.
Upon oral administration, soquelitinib selectively and covalently binds to the cysteine
residue at position 442 (CYS-442) of ITK, thereby disrupting ITK-mediated signal transduction,
while sparing tyrosine-protein kinase TXK (resting lymphocyte kinase, RLK) activity.
This may abrogate T-cell receptor (TCR) signaling through ITK and inhibit TCR-induced
proliferation of malignant T-cells. Additionally, inhibiting ITK activation may prevent
the upregulation of GATA-3, a transcription factor that drives T-helper 2 (Th2) cell
differentiation and is overexpressed in certain T-cell lymphomas. Thus, selective
inhibition of ITK may inhibit Th2 responses without affecting T-helper 1 (Th1)-dependent
immunity. ITK, a member of the Tec family of non-receptor protein tyrosine kinases
plays a significant role in the T-cell development, differentiation and production
of pro-inflammatory cytokines.;
UNII : 6I5H17AN3I;
CAS number : 2226636-04-8;
Molecule name : CPI-818; CPI 818;
NCI Metathesaurus CUI : CL970662;
Origin ID : C162010;
UMLS CUI : C5908083;
Semantic type(s)
- concept_is_in_subset
- has_target
