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Numidargistat (CB-1158) (INCB01158) is an orally bioavailable, potent (IC50 = 98 nM), and selective (minimal off-target activity at 50000 nM) inhibitor of human arginase I, an immune-mediated anti-tumor agent. L-arginine is a critical metabolite for T-cell receptor signaling and subsequent T-cell proliferation, and depletion of arginine arrests T-cell growth. In the tumor microenvironment, infiltrating myeloid-derived suppressor cells (MDSCs), macrophages, and neutrophils produce arginase, which depletes local arginine concentrations and dampens T cell-mediated immune surveillance. Pharmacological inhibition of arginase is expected to restore arginine levels and allow T-cells to proliferate, thereby leading to an immune-mediated anti-tumor response. In culture, human granulocytes release arginase and deplete media arginine to levels that inhibit T-cell proliferation. In a co-culture system of human granulocytes and T-cells, CB-1158 potently blocks granulocyte-derived arginase activity, maintains extracellular arginine levels, and restores proliferation of T-cells (ref. 1). CB-1158 has single agent efficacy in mouse tumor models and synergistically enhances the antitumor efficacy of checkpoint inhibitors (ref. 2).
Catalog NO: CT-CB1158
Synonym: CB-1158, INCB01158
CAS NO: 2095732-06-0
Mol. Formula: C11H22BN3O5 ∙ 2HC
MW: 360.0 (or refer to Certificate of Analysis, batch-specific)
** Good-looking white crystals (pic attached), in vivo QUALITY material. 99% by Achiral and Chiral HPLCs. Stereochemistry is validated by 3D X-Ray Structure (Ref. 3a). Validated Hydrochloride salt (Ref. 3b). Bulk (Get quote). Same Day Shipping.