Numidargistat
Based on 12 publication(s) in Google Scholar
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.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.0%
- CAS 番号: 2095732-06-0
- 分子式: C11H22BN3O5
- 分子量:287.12
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
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MedChemExpress（MCE）の使用を引用している文献 Numidargistat
More- Cancer Cell. 2025 Feb 10;43(2):269-291.e19. [Abstract]
- Cell Death Dis. 2025 Dec 21. [Abstract]
- Cancer Lett. 2023 Jun 28:564:216208. [Abstract]
- Cell Commun Signal. 2023 Sep 18;21(1):236. [Abstract]
- Cancer Immunol Res. 2026 May 4;14(5):875-891. [Abstract]
- J Physiol. 2020 Nov;598(21):4907-4925. [Abstract]
- Res Sq. 2026 Feb 24.
- Patent. US20240307497A1.
- bioRxiv. 2024 Jul 31:2023.09.06.556606. [Abstract]
- The University of Chicago. 2023 Dec.
- Biomed Pharmacother. 2022 Sep:153:113321. [Abstract]
- Research Square Preprint. 2022 Mar.
Customer Validation & Images
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Cell Proliferation/Viability Assay
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RT-PCR
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Bio/Physico-chemical Assay
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Cell Imaging/Staining
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Flow Cytometry
生物活性
IC50: 86 nM (Arginase 1), 296 nM (Arginase 2)[1]
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 2095732-06-0
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性状 Solid
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分子量 287.12
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分子式 C11H22BN3O5
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Color Off-white to light yellow
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SMILES
O=C([C@@H](N)C)N1C[C@H](CCCB(O)O)[C@](N)(C(O)=O)C1
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別名
CB-1158; INCB01158
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (12)
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Journal Impact Factor
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Most Recent
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Cancer Cell
Adiponectin reduces immune checkpoint inhibitor-induced inflammation without blocking anti-tumor immunity. [Abstract]2025 Feb 10;43(2):269-291.e19. PMID: 39933899 -
Cell Death Dis
Tubule-derived CCN1 drives renal repair via αvβ5-STAT6-ARG1-dependent reprogramming of macrophages. [Abstract]2025 Dec 21. PMID: 41422302
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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Cancer Lett
Myeloid-derived suppressor cells deficient in cholesterol biosynthesis promote tumor immune evasion. [Abstract]2023 Jun 28:564:216208. PMID: 37150500 -
Cell Commun Signal
Arginase-1 promotes lens epithelial-to-mesenchymal transition in different models of anterior subcapsular cataract. [Abstract]2023 Sep 18;21(1):236. PMID: 37723490 -
Cancer Immunol Res
CLK1 Promotes Myeloid-Derived Suppressor Cell Trafficking and Reprograms the Tumor Microenvironment by Activating Hippo/YAP Signaling in Colorectal Cancer. [Abstract]2026 May 4;14(5):875-891. PMID: 41686262
Numidargistat purchased from MedChemExpress. Usage Cited in: Cancer Immunol Res. 2026 May 4;14(5):875-891. [Abstract]
Numidargistat (CB-1158) (10 µM; 48 h) significantly reversed the immunosuppressive effect on CD8+ T-cell proliferation.
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J Physiol
Arginase 1 is involved in lacrimal hyposecretion in male NOD mice, a model of Sjögren's syndrome, regardless of dacryoadenitis status. [Abstract]2020 Nov;598(21):4907-4925. PMID: 32780506 -
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bioRxiv
Myeloid-mesenchymal crosstalk drives Arg1-dependent profibrotic metabolism via ornithine in lung fibrosis. [Abstract]2024 Jul 31:2023.09.06.556606. PMID: 39211079 -
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Biomed Pharmacother
Muscarinic acetylcholine receptors regulate inflammatory responses through arginases 1/2 in zebrafish. [Abstract]2022 Sep:153:113321. PMID: 35759868 -
溶剤 & 溶解度
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
プロトコル
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (281 KB)
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参考文献
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| 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 関連分類
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