Numidargistat (Synonyms: CB-1158; INCB01158)

Name: Numidargistat
Brand: MedChemExpress
SKU: HY-101979
Rating: 5.0 (12 reviews)

Cat. No.: HY-101979 Purity: 98.0%: Data Sheet
COA

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Handling Instructions
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Numidargistat (CB-1158) is a potent and orally active inhibitor of arginase, with IC₅₀s of 86 nM and 296 nM for recombinant human arginase 1 and recombinant human arginase 2, respectively. Immuno-oncology agent.

For research use only. We do not sell to patients.

CAS No. : 2095732-06-0

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 12 publication(s) in Google Scholar

Other Forms of Numidargistat:

Numidargistat dihydrochloride In-stock
Numidargistat (Standard) Get quote

12 Publications Citing Use of MCE Numidargistat

RT-PCR

Cell Proliferation/Viability Assay

Bio/Physico-chemical Assay

Cell Imaging/Staining

Flow Cytometry

: Numidargistat purchased from MedChemExpress. Usage Cited in: Cancer Immunol Res. 2026 May 4;14(5):875-891.; Numidargistat (CB-1158) (10 µM; 48 h) significantly reversed the immunosuppressive effect on CD8⁺ T-cell proliferation.

: Numidargistat purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2025 Dec 21. [Abstract]; Numidargistat (50 μM; 48 h) significantly inhibited the upregulation of mRNA levels of growth factors including Igf1, Pdgfb, and Vegfa that were induced by CCN1 treatment in BMDMs.

: Numidargistat purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2025 Dec 21. [Abstract]; Numidargistat (50 μM; 48 h) suppressed the concentration of growth factors IGF-1 and PDGF-BB released from CCN1-treated BMDMs.

: Numidargistat purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2025 Dec 21. [Abstract]; Numidargistat (50 μM; 48 h) inhibited CCN1-induced increase in EdU⁺ proliferating cells in HK-2 cells co-cultured with BMDMs.

: Numidargistat purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2025 Dec 21. [Abstract]; Numidargistat (50 μM; 48 h) significantly decreased the proportion of EdU⁺ HK-2 cells in BMDMs.

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Protocol
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Description

IC₅₀ & Target

IC50: 86 nM (Arginase 1), 296 nM (Arginase 2)^[1]

In Vitro

Numidargistat is a potent and orally-bioavailable inhibitor of arginase, with IC₅₀s of 86 and 296 nM for recombinant human arginase 1 and 2, respectively. Numidargistat inhibits native rginase 1 (Arg1) in human granulocyte, erythrocyte, and hepatocyte lysate with IC₅₀s of 178 nM, 116 nM and 158 nM, respectively, and blocks Arg1 in cancer patient plasma (IC₅₀, 122 nM). Numidargistat also exhibits potent inhibitory activity against arginase in human HepG2, K562 cell lines and primary human hepatocytes with IC₅₀s of 32, 139, 210 μM, respectively. Numidargistat show no effect on NOS. In addition, Numidargistat is not directly cytotoxic to murine cancer cell lines^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Numidargistat (100 mg/kg, p.o., twice per day) increases the number of tumor-infiltrating cytotoxic cells and decreases myeloid cells in mice. Numidargistat in combination with PD-L1 blockade or gemcitabine inhibits tumor growth in mice bearing CT26 cancer cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

287.12

Formula

C₁₁H₂₂BN₃O₅

CAS No.

2095732-06-0

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

H₂O : 100 mg/mL (348.29 mM; Need ultrasonic)

DMSO : 100 mg/mL (348.29 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.4829 mL	17.4143 mL	34.8286 mL
5 mM	0.6966 mL	3.4829 mL	6.9657 mL
10 mM	0.3483 mL	1.7414 mL	3.4829 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (8.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 98.91%

Select Batch:

Data Sheet (281 KB) SDS (252 KB)

COA (252 KB) HNMR (128 KB) RP-HPLC (212 KB) MS (69 KB)

Handling Instructions (2659 KB)

References

[1]. Steggerda SM, et al. Inhibition of arginase by CB-1158 blocks myeloid cell-mediated immune suppression in the tumor microenvironment. J Immunother Cancer. 2017 Dec 19;5(1):101. [Content Brief]

Cell Assay ^[1]	Intracellular arginase activity is determined for the arginase-expressing HepG2 and K-562 cell lines as follows. HepG2 cells are seeded at 100,000 cells per well one day prior to treatment with CB-1158. K-562 cells are seeded at 200,000 cells per well on the day of CB-1158 treatment. Cells are treated with a dose-titration of CB-1158 in SILAC RPMI-1640 media containing 5% heat-inactivated and dialyzed FBS, antibiotics/anti-mycotic, 10 mM L-arginine, 0.27 mM L-lysine, and 2 mM L-glutamine. The medium is harvested after 24 h and urea generated is determined. Wells containing media without cells are used as background controls. For assessing the effect of CB-1158 on Arg1 in primary hepatocytes, frozen human hepatocytes are thawed, allowed to adhere onto collagen-coated wells for 4 h, and then incubated for 48 h in SILAC-RPMI containing 10 mM L-ornithine, no L-arginine, and a dose-titration of CB-1158, at which time the media are analyzed for urea^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice^[1] For the 4T1 tumor model, 10⁵ cells are injected orthotopically into the mammary fat pad; for all other tumor models, 10⁶ cells are injected subcutaneously (s.c.) in the right flank. For all studies, CB-1158 is administered by oral gavage twice per day at 100 mg/kg starting on study day 1 (1 day after tumor implant). Control groups receive vehicle (water) twice daily by gavage. Tumor volume measured by digital caliper (length × width × width/2) and body weight are recorded three times per week. Mice are euthanized when tumors necrotize or volumes reach 2000 mm³. For the CT26 model, anti-PD-L1 antibody (5 mg/kg) is injected intraperitoneally (i.p.) on days 5, 7, 9, 11, 13, and 15. For the 4T1 model, anti-CTLA-4 antibody (5 mg/kg) is injected i.p. on days 2, 5, and 8; anti-PD-1 antibody (5 mg/kg) is injected i.p. on days 3, 6, and 9. 4T1 tumors are harvested on study day 25 into Fekete’s solution and tumor nodules are enumerated visually. Gemcitabine is dosed 50 mg/kg i.p. on days 10 and 16 for the CT26 model, 60 mg/kg i.p. on days 6 and 10 for the LLC model, or 30 mg/kg i.p. on day 5 for the 4T1 model. With these regimens, gemcitabine modestly reduces tumor growth and spares most tumor-infiltrating immune cells, allowing for the evaluation of combination activity with CB-1158^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Steggerda SM, et al. Inhibition of arginase by CB-1158 blocks myeloid cell-mediated immune suppression in the tumor microenvironment. J Immunother Cancer. 2017 Dec 19;5(1):101. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	3.4829 mL	17.4143 mL	34.8286 mL	87.0716 mL
	5 mM	0.6966 mL	3.4829 mL	6.9657 mL	17.4143 mL
	10 mM	0.3483 mL	1.7414 mL	3.4829 mL	8.7072 mL
	15 mM	0.2322 mL	1.1610 mL	2.3219 mL	5.8048 mL
	20 mM	0.1741 mL	0.8707 mL	1.7414 mL	4.3536 mL
	25 mM	0.1393 mL	0.6966 mL	1.3931 mL	3.4829 mL
	30 mM	0.1161 mL	0.5805 mL	1.1610 mL	2.9024 mL
	40 mM	0.0871 mL	0.4354 mL	0.8707 mL	2.1768 mL
	50 mM	0.0697 mL	0.3483 mL	0.6966 mL	1.7414 mL
	60 mM	0.0580 mL	0.2902 mL	0.5805 mL	1.4512 mL
	80 mM	0.0435 mL	0.2177 mL	0.4354 mL	1.0884 mL
	100 mM	0.0348 mL	0.1741 mL	0.3483 mL	0.8707 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Numidargistat Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Numidargistat2095732-06-0CB-1158 INCB01158CB1158CB 1158INCB01158INCB 01158INCB-01158ArginaseInhibitorinhibitorinhibit

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Numidargistat (Synonyms: CB-1158; INCB01158)

Customer Review

Other Forms of Numidargistat:

Numidargistat Related Antibodies

12 Publications Citing Use of MCE Numidargistat

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•Related Screening Libraries:

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Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Numidargistat Related Antibodies

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Complete Stock Solution Preparation Table

Numidargistat Related Classifications

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