| Field | Specification |
|---|---|
| Alternative names | CB-1158; INCB01158 |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C11H22BN3O5 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Numidargistat, also known as CB-1158 or INCB01158, is a potent, orally active inhibitor of arginase, with IC50 values of 86 nM for recombinant human arginase 1 and 296 nM for recombinant human arginase 2. It is described as an immuno-oncology agent[1]. It is supplied as an off-white to light yellow solid (C11H22BN3O5, MW 287.12) at 98.0% purity.
Physical & Chemical Properties
| CAS Number | 2095732-06-0 |
|---|---|
| Molecular Formula | C11H22BN3O5 |
| Molecular Weight | 287.12 g/mol |
| Purity | 98.0% |
| Appearance | Solid |
| Color | Off-white to light yellow |
| SMILES | O=C([C@@H](N)C)N1C[C@H](CCCB(O)O)[C@](N)(C(O)=O)C1 |
| Signaling Pathway | Immunology/Inflammation; Metabolic Enzyme/Protease |
| Solubility | In Vitro: H2O: 100 mg/mL (348.29 mM; Requires sonication) DMSO: 100 mg/mL (348.29 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target
IC50: 86 nM (Arginase 1), 296 nM (Arginase 2)[1]
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| H2O | 100 mg/mL (348.29 mM) | requires sonication |
| DMSO | 100 mg/mL (348.29 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); avoid repeated freeze-thaw cycles.
If water is used as the stock solvent, dilute to the working solution and sterilize it through a 0.22 μm filter before use.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.5 mg/mL (8.71 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 2.5 mg/mL (8.71 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.5 mg/mL (8.71 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
Numidargistat is a potent, orally-bioavailable arginase inhibitor. Recombinant human arginase 1 and 2 are inhibited with IC50s of 86 and 296 nM, respectively. Native arginase 1 (Arg1) in human granulocyte, erythrocyte, and hepatocyte lysate is inhibited by Numidargistat, with IC50s of 178 nM, 116 nM and 158 nM, respectively; Numidargistat also blocks Arg1 in cancer patient plasma (IC50, 122 nM). Numidargistat also shows potent inhibitory activity against arginase in human HepG2 and K562 cell lines and in primary human hepatocytes, with IC50s of 32, 139, 210 μM, respectively. It has no effect on NOS. Numidargistat is also not directly cytotoxic to murine cancer cell lines[1].
In Vivo
In mice, Numidargistat (100 mg/kg, p.o., twice per day) raises the number of tumor-infiltrating cytotoxic cells and lowers myeloid cells. Combined with PD-L1 blockade or gemcitabine, Numidargistat inhibits tumor growth in mice bearing CT26 cancer cells[1].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
Cell Assay[1]
Measure intracellular arginase activity in the arginase-expressing HepG2 and K-562 cell lines as follows. Seed HepG2 cells at 100,000 cells per well one day before treatment with CB-1158. Seed K-562 cells at 200,000 cells per well on the day of CB-1158 treatment. Treat cells with CB-1158 as a dose-titration in SILAC RPMI-1640 media supplemented with 10 mM L-arginine, 0.27 mM L-lysine, and 2 mM L-glutamine, plus 5% heat-inactivated and dialyzed FBS and antibiotics/anti-mycotic. Harvest the medium after 24 h and determine the urea generated. Use wells containing media without cells as background controls. To assess the effect of CB-1158 on Arg1 in primary hepatocytes, thaw frozen human hepatocytes, allow them to adhere onto collagen-coated wells for 4 h, then incubate in SILAC-RPMI with 10 mM L-ornithine, no L-arginine, and a dose-titration of CB-1158 for 48 h; at that point, analyze the media for urea[1].
Animal Administration[1]
Mice[1]: For the 4T1 tumor model, inject 105 cells orthotopically into the mammary fat pad; for every other tumor model, inject 106 cells subcutaneously (s.c.) into the right flank. In all studies, give CB-1158 at 100 mg/kg by oral gavage twice per day, beginning on study day 1 (1 day after tumor implant). Give control groups vehicle (water) by gavage, also twice daily. Record tumor volume, measured with a digital caliper (length × width × width/2), and body weight three times per week. Euthanize mice when tumors necrotize or volumes reach 2000 mm3. For the CT26 model, inject anti-PD-L1 antibody (5 mg/kg) intraperitoneally (i.p.) on days 5, 7, 9, 11, 13, and 15. For the 4T1 model, inject i.p. anti-CTLA-4 antibody (5 mg/kg) on days 2, 5, and 8, and anti-PD-1 antibody (5 mg/kg) on days 3, 6, and 9. Harvest 4T1 tumors on study day 25 into Fekete’s solution and count the tumor nodules visually. Dose gemcitabine i.p. at 50 mg/kg on days 10 and 16 in the CT26 model, at 60 mg/kg on days 6 and 10 in the LLC model, and at 30 mg/kg on day 5 in the 4T1 model. Under these regimens, tumor growth is reduced only modestly by gemcitabine and most tumor-infiltrating immune cells are spared, which allows combination activity with CB-1158 to be evaluated[1].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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CLK1 Promotes Myeloid-Derived Suppressor Cell Trafficking and Reprograms the Tumor Microenvironment by Activating Hippo/YAP Signaling in Colorectal Cancer. Cancer Immunol Res 2026 May 4;14(5):875-891. PMID: 41686262
Arginase 1 is involved in lacrimal hyposecretion in male NOD mice, a model of Sjögren's syndrome, regardless of dacryoadenitis status. J Physiol 2020 Nov;598(21):4907-4925. PMID: 32780506
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Myeloid-mesenchymal crosstalk drives Arg1-dependent profibrotic metabolism via ornithine in lung fibrosis. bioRxiv 2024 Jul 31:2023.09.06.556606. PMID: 39211079
The University of Chicago. 2023 Dec.
