INCB-024360 (Synonyms: INCB024360) |
Catalog No.GC17968
One-Click Copy Product Info
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INCB-024360, also known as epacadostat, is an oral small molecule selective IDO1 inhibitor (IC50 = 71.8nM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1204669-58-8
Sample solution is provided at 25 µL, 10mM.
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INCB-024360, also known as epacadostat, is an oral small molecule selective IDO1 inhibitor (IC50 = 71.8nM) [1]. INCB-024360 can selectively inhibit IDO1 enzyme activity and block the pathway of tryptophan metabolism to kynurenine [2]. INCB-024360 is mainly used to treat advanced or metastatic solid tumors [3-4].
In SKOV-3 cells, INCB-024360 (10-3-104nM; 24h, 48h, 72h) increases IDO1 protein expression [5]. In HT-29 cells, INCB-024360 (10μM; 96h) reduced cell viability [6]. In 4T1 cells, INCB-024360 (1μM; 24h, 48h) sensitize pulmonary metastases to agents targeting hypoxia/nutrient deprivation survival mechanisms [7].
In colon carcinoma xenograft mice model, INCB-024360 (100mg/kg; ig; 2h) effectively inhibits the metabolism of tryptophan to kynurenine by achieving high drug exposure in areas with high IDO1 expression, significantly reducing the Kyn/Trp ratio, thereby restoring immune activity and enhancing anti-tumor efficacy [8]. In in wild-type and PD-1-negative mice, co-administration of the CTLA-4 blocking antibody 9D9 and/or the IDO1 inhibitor INCB-024360 (300mg/kg; ig; 27d) (to mimic the effects of PD1 blockade) synergistically induced liver injury and immune cell infiltration [9]. In TAC-induced WT mice, INCB-024360 (50mg/kg; sc; 4 weeks) inhibits IDO1 and ameliorates pathological cardiac hypertrophy and remodeling [10].
References:
[1]. Liu X, Shin N, Koblish HK, et al. Selective inhibition of IDO1 effectively regulates mediators of antitumor immunity. Blood, The Journal of the American Society of Hematology. 2010 Apr 29; 115(17): 3520-3230.
[2]. Hao X, Chen Z, Li H, et al. Small-molecule drugs in immunotherapy. Mini Reviews in Medicinal Chemistry. 2023 Jul 1;23(13):1341-1359.
[3]. Alford B, Cox K, Soliman H. IDO1 inhibitors for cancer immunotherapy. Drugs of the Future. 2016 Sep 1; 41(9): 553-559.
[4]. Hellmann MD, Gettinger S, Chow LQ, et al. Phase 1 study of epacadostat in combination with atezolizumab for patients with previously treated advanced nonsmall cell lung cancer. International Journal of Cancer. 2020 Oct 1; 147(7): 1963-1969.
[5]. Rossini S, Ambrosino S, Volpi C, et al. Epacadostat stabilizes the apo-form of IDO1 and signals a pro-tumorigenic pathway in human ovarian cancer cells. Frontiers in Immunology. 2024 Jan 25; 15: 1346686.
[6]. Zhou Y, Tao Q, Luo C, et al. Epacadostat Overcomes Cetuximab Resistance in Colorectal Cancer by Targeting IDO‐Mediated Tryptophan Metabolism. Cancer Science. 2025 Mar 18.
[7]. Shen SC, Dey S, DuHadaway JB, et al. Neovascular pruning by IDO1 inhibitors can potentiate immunogenic cytotoxicity of ischemia-targeted agents to synergistically enhance anti-PD-1 responsiveness. Journal for Immunotherapy of Cancer. 2025 May 30; 13(5): e011398.
[8]. Poncelet L, Ait-Belkacem R, Marillier R, et al. Target exposure and pharmacodynamics study of the indoleamine 2, 3-dioxygenase-1 (IDO-1) inhibitor epacadostat in the CT26 mouse tumor model. Journal of Pharmaceutical and Biomedical Analysis. 2019 Jun 5; 170: 220-227.
[9]. Affolter T, Llewellyn HP, Bartlett DW, et al. Inhibition of immune checkpoints PD-1, CTLA-4, and IDO1 coordinately induces immune-mediated liver injury in mice. PLoS One. 2019 May 21; 14(5): e0217276.
[10]. Wang Y, Song J, Yu K, et al. Indoleamine 2, 3-dioxygenase 1 deletion-mediated kynurenine insufficiency inhibits pathological cardiac hypertrophy. Hypertension. 2023 Oct; 80(10): 2099-2111.
| Cell experiment [1]: | |
Cell lines | SKOV-3 cells |
Preparation Method | The cell viability of SKOV-3 cells exposed to INCB-024360 was analyzed by MTT assay. Cells were seeded at the final concentration of 5 x 103 cells/100µL/well in a 96-well plate, and treated with INCB-024360 for 24, 48, and 72 hours. Vehicle-treated cells were used as control. At each time point, the stimulus was removed and cells were provided with 110µL/well of complete medium containing MTT at the final concentration of 0.45mg/mL. After 4 hours at 37℃, 100µL/well of the solubilization buffer (SDS 10% in HCl 0.01M) were added and cells were incubated overnight at 37℃. The day after, cell viability was determined by measuring the absorbance at 570nm, by using a UV/visible spectrophotometer. |
Reaction Conditions | 10-3-104nM; 24h, 48h, 72h |
Applications | INCB-024360 increases IDO1 protein expression in SKOV-3 cells. |
| Animal experiment [2]: | |
Animal models | Colon carcinoma xenograft mice model |
Preparation Method | Colon carcinoma CT26 cell line was subcutaneously grafted into BALB/c mice (Charles River Laboratories, France). Mice were randomized and treatment was started when tumors had an average size of 70-120mm3. Mice were treated by oral gavage with the IDO1 inhibitor, INCB-024360 at 100mg/kg, and then sacrificed 2h later. |
Dosage form | 100mg/kg; ig; 2h |
Applications | INCB-024360 effectively inhibits the metabolism of tryptophan to kynurenine by achieving high drug exposure in areas with high IDO1 expression, significantly reducing the Kyn/Trp ratio, thereby restoring immune activity and enhancing anti-tumor efficacy. |
References: | |
| Cas No. | 1204669-58-8 | SDF | |
| Synonyms | INCB024360 | ||
| Chemical Name | (E)-N'-(3-bromo-4-fluorophenyl)-N-hydroxy-4-((2-(sulfamoylamino)ethyl)amino)-1,2,5-oxadiazole-3-carboximidamide | ||
| Canonical SMILES | BrC1=C(F)C=CC(/N=C(NO)\C2=NON=C2NCCNS(N)(=O)=O)=C1 | ||
| Formula | C11H13BrFN7O4S | M.Wt | 438.23 |
| Solubility | ≥ 17.1mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.2819 mL | 11.4095 mL | 22.8191 mL |
| 5 mM | 456.4 μL | 2.2819 mL | 4.5638 mL |
| 10 mM | 228.2 μL | 1.141 mL | 2.2819 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 26 reference(s) in Google Scholar.)