製品番号: HY-15689

Epacadostat

(別名: INCB 024360)

28 Cited Publications

カスタマーレビュー

Based on 28 publication(s) in Google Scholar

Epacadostat (INCB 024360) is a potent and selective indoleamine 2,3-dioxigenase 1 (IDO1) inhibitor with an IC₅₀ of 71.8 nM. Epacadostat can effectively reduce Trp metabolism, entailing increased activation and maturation of dendritic cells, and enhanced proliferation of effector T cells and natural killer cells (NKs), as well as attenuated Tregs expansion.

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純度: 99.72%
CAS 番号: 1204669-58-8
分子式: C₁₁H₁₃BrFN₇O₄S
分子量:438.23

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Epacadostat 構造式

CAS 番号: 1204669-58-8

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生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
- 臨床実験
化学情報
Publications (28)
溶剤 & 溶解度
- 体外
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純度とドキュメンテーション
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生物活性

製品説明

Epacadostat (INCB 024360) is a potent and selective indoleamine 2,3-dioxigenase 1 (IDO1) inhibitor with an IC₅₀ of 71.8 nM^[1]. Epacadostat can effectively reduce Trp metabolism, entailing increased activation and maturation of dendritic cells, and enhanced proliferation of effector T cells and natural killer cells (NKs), as well as attenuated Tregs expansion.

IC₅₀ & Target^[1]

IDO1

71.8 nM (IC₅₀)

Indoleamine 2,3-Dioxygenase (IDO) アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	>100 μM Compound: 2; INCB024360	Antiproliferative activity against human A549 cells after 48 hrs by CCK-8 assay Antiproliferative activity against human A549 cells after 48 hrs by CCK-8 assay	[PMID: 29670692]
A549	IC₅₀	>50 μM Compound: Epacadostat	Cytotoxicity against human A549 cells measured after 48 hrs by MTT assay Cytotoxicity against human A549 cells measured after 48 hrs by MTT assay	[PMID: 37060754]
A549	IC₅₀	34.53 μM Compound: 7; INCB24360	Antiproliferative activity against NAMPT inhibitor-resistant A549 cells assessed as reduction in cell viability measured for 48 hrs in presence of FK866 by CCK-8 assay Antiproliferative activity against NAMPT inhibitor-resistant A549 cells assessed as reduction in cell viability measured for 48 hrs in presence of FK866 by CCK-8 assay	[PMID: 36595482]
A549	IC₅₀	61.06 μM Compound: 7; INCB24360	Antiproliferative activity against NAMPT inhibitor-resistant A549 cells assessed as reduction in cell viability measured for 48 hrs by CCK-8 assay Antiproliferative activity against NAMPT inhibitor-resistant A549 cells assessed as reduction in cell viability measured for 48 hrs by CCK-8 assay	[PMID: 36595482]
CT26	IC₅₀	>100 μM Compound: 1	Cytotoxicity against mouse CT26 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay Cytotoxicity against mouse CT26 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay	[PMID: 33482599]
CT26	IC₅₀	>100 μM Compound: 2; INCB024360	Antiproliferative activity against mouse CT26 cells after 48 hrs by CCK-8 assay Antiproliferative activity against mouse CT26 cells after 48 hrs by CCK-8 assay	[PMID: 29670692]
CT26	IC₅₀	1.49 μM Compound: Epacadostat	Cytotoxicity against mouse CT26 cells incubated for 48 hrs by CCK-8 assay Cytotoxicity against mouse CT26 cells incubated for 48 hrs by CCK-8 assay	[PMID: 36370550]
CT26	IC₅₀	47.09 μM Compound: Epacadostat	Cytotoxicity against mouse CT26 cells assessed as reduction in cell viability by CCK8 assay Cytotoxicity against mouse CT26 cells assessed as reduction in cell viability by CCK8 assay	[PMID: 34854662]
CT26	IC₅₀	64.6 μM Compound: 1; INCB24360	Cytotoxicity against mouse CT26 cells assessed as cell viability measured after 24 hrs by CCK-8 assay Cytotoxicity against mouse CT26 cells assessed as cell viability measured after 24 hrs by CCK-8 assay	[PMID: 36842272]
HCT-116	IC₅₀	>100 μM Compound: 2; INCB024360	Antiproliferative activity against human HCT116 cells after 48 hrs by CCK-8 assay Antiproliferative activity against human HCT116 cells after 48 hrs by CCK-8 assay	[PMID: 29670692]
HCT-116	IC₅₀	>50 μM Compound: Epacadostat	Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 34147748]
HCT-116	IC₅₀	>50 μM Compound: Epacadostat	Cytotoxicity against human HCT-116 cells measured after 48 hrs by MTT assay Cytotoxicity against human HCT-116 cells measured after 48 hrs by MTT assay	[PMID: 37060754]
HCT-116	IC₅₀	0.26 μM Compound: Epacadostat	Cytotoxicity against human HCT-116 cells incubated for 48 hrs by CCK-8 assay Cytotoxicity against human HCT-116 cells incubated for 48 hrs by CCK-8 assay	[PMID: 36370550]
HCT-116	IC₅₀	36.3 μM Compound: 1; INCB24360	Cytotoxicity against human HCT-116 cells assessed as cell viability measured after 24 hrs by CCK-8 assay Cytotoxicity against human HCT-116 cells assessed as cell viability measured after 24 hrs by CCK-8 assay	[PMID: 36842272]
HCT-116	IC₅₀	37.1 μM Compound: Epacadostat	Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability by CCK8 assay Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability by CCK8 assay	[PMID: 34854662]
HEK293	IC₅₀	0.242 μM Compound: INCB024360	Inhibition of TDO (unknown origin) expressed in HEK293 cells using L-Trp as substrate after 8 hrs Inhibition of TDO (unknown origin) expressed in HEK293 cells using L-Trp as substrate after 8 hrs	[PMID: 30321802]
HEK293	IC₅₀	0.26 μM Compound: INCB24360	Inhibition of human TDO transfected in HEK293 cells assessed as reduction in kynurenine production using L-tryptophan as substrate incubated for 12 hrs Inhibition of human TDO transfected in HEK293 cells assessed as reduction in kynurenine production using L-tryptophan as substrate incubated for 12 hrs	[PMID: 31580660]
HEK293	IC₅₀	12.6 nM Compound: 1	Inhibition of recombinant human IDO1 expressed in HEK293 cells assessed as N-formylkynurenine formation by measuring kynurenine level incubated for 12 hrs by microplate reader analysis Inhibition of recombinant human IDO1 expressed in HEK293 cells assessed as N-formylkynurenine formation by measuring kynurenine level incubated for 12 hrs by microplate reader analysis	[PMID: 31233921]
HeLa	EC₅₀	0.013 μM Compound: INCB024360	Inhibition of IFNgamma-stimulated IDO1 in human HeLa cells Inhibition of IFNgamma-stimulated IDO1 in human HeLa cells	[PMID: 31882299]
HeLa	EC₅₀	7.4 nM Compound: INCB024360	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability Antiproliferative activity against human HeLa cells assessed as reduction in cell viability	[PMID: 33569941]
HeLa	EC₅₀	8 nM Compound: Epacadostat	Inhibition of IDO1 in IFN-gamma stimulated human HeLa cells assessed as reduction in kynurenine formation using L-tryptophan as substrate incubated for 24 hrs by UV-spectrophotometry Inhibition of IDO1 in IFN-gamma stimulated human HeLa cells assessed as reduction in kynurenine formation using L-tryptophan as substrate incubated for 24 hrs by UV-spectrophotometry	[PMID: 32088128]
HeLa	IC₅₀	>100 μM Compound: 1	Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay	[PMID: 33482599]
HeLa	IC₅₀	>50 μM Compound: Epacadostat	Cytotoxicity against human HeLa cells measured after 48 hrs by MTT assay Cytotoxicity against human HeLa cells measured after 48 hrs by MTT assay	[PMID: 37060754]
HeLa	IC₅₀	0.007 μM Compound: INCB24360	Inhibition of IDO1 in IFN-gamma stimulated human HeLa cells assessed as reduction in kynurenine production incubated for 18 hrs Inhibition of IDO1 in IFN-gamma stimulated human HeLa cells assessed as reduction in kynurenine production incubated for 18 hrs	[PMID: 31580660]
HeLa	IC₅₀	0.016 μM Compound: Epacadostat	Inhibition of IDO1 in IFN-gamma stimulated human HeLa cells assessed as reduction in kynurenine production using L-tryptophan as substrate incubated for 24 hrs Inhibition of IDO1 in IFN-gamma stimulated human HeLa cells assessed as reduction in kynurenine production using L-tryptophan as substrate incubated for 24 hrs	[PMID: 31610376]
HeLa	IC₅₀	0.02 μM Compound: INCB024360	Inhibition of IDO1 in human HeLa cells Inhibition of IDO1 in human HeLa cells	[PMID: 32247733]
HeLa	IC₅₀	0.07 μM Compound: INCB24360	Inhibition of IDO1 in human HeLa cells using L-tryptophan as substrate after 20 hrs Inhibition of IDO1 in human HeLa cells using L-tryptophan as substrate after 20 hrs	[PMID: 30469041]
HeLa	IC₅₀	10 nM Compound: 1; INCB24360	Inhibition of IDO1 in human HeLa cells using L-tryptophan as substrate incubated for 48 hrs Inhibition of IDO1 in human HeLa cells using L-tryptophan as substrate incubated for 48 hrs	[PMID: 31445231]
HeLa	IC₅₀	10.3 nM Compound: INCB024360	Inhibition of IDO1 in IFN-gamma stimulated human HeLa cells assessed as reduction in kynurenine production incubated for 24 hrs relative to control Inhibition of IDO1 in IFN-gamma stimulated human HeLa cells assessed as reduction in kynurenine production incubated for 24 hrs relative to control	[PMID: 30858027]
HeLa	IC₅₀	12.5 nM Compound: Epacadostat	Inhibition of IDO1 in IFN-gamma stimulated human HeLa cells using L-tryptophan as substrate incubated for 48 hrs by fluorescence assay Inhibition of IDO1 in IFN-gamma stimulated human HeLa cells using L-tryptophan as substrate incubated for 48 hrs by fluorescence assay	[PMID: 32832022]
HeLa	IC₅₀	4.63 μM Compound: Epacadostat	Cytotoxicity against human HeLa cells incubated for 48 hrs by CCK-8 assay Cytotoxicity against human HeLa cells incubated for 48 hrs by CCK-8 assay	[PMID: 36370550]
HeLa	IC₅₀	59.8 μM Compound: 1; INCB24360	Cytotoxicity against human HeLa cells assessed as cell viability measured after 24 hrs by CCK-8 assay Cytotoxicity against human HeLa cells assessed as cell viability measured after 24 hrs by CCK-8 assay	[PMID: 36842272]
HeLa	IC₅₀	7.1 nM Compound: 1; INCB024360	Inhibition of IFN-gamma-stimulated IDO1 activity in human HeLa cells using L-tryptophan as substrate after 48 hrs by microplate reader analysis Inhibition of IFN-gamma-stimulated IDO1 activity in human HeLa cells using L-tryptophan as substrate after 48 hrs by microplate reader analysis	[PMID: 25970480]
HeLa	IC₅₀	7.1 nM Compound: INCB24360	Inhibition of IFN-gamma stimulated IDO1 in human HeLa cells assessed as reduction in formation of kynurenine incubated for 48 hrs in presence of IFNgamma by microplate reader assay Inhibition of IFN-gamma stimulated IDO1 in human HeLa cells assessed as reduction in formation of kynurenine incubated for 48 hrs in presence of IFNgamma by microplate reader assay	[PMID: 31580660]
HeLa	IC₅₀	7.4 nM Compound: 4f; INCB24360	Inhibition of IDO1 in IFN-gamma-stimulated human HeLa cells assessed as decrease in kynurenine levels after 48 hrs Inhibition of IDO1 in IFN-gamma-stimulated human HeLa cells assessed as decrease in kynurenine levels after 48 hrs	[PMID: 28523098]
HepG2	IC₅₀	>50 μM Compound: Epacadostat	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 34147748]
HGC-27	IC₅₀	>50 μM Compound: Epacadostat	Cytotoxicity against human HGC-27 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Cytotoxicity against human HGC-27 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 34147748]
HT-29	IC₅₀	>100 μM Compound: 2; INCB024360	Antiproliferative activity against human HT-29 cells after 48 hrs by CCK-8 assay Antiproliferative activity against human HT-29 cells after 48 hrs by CCK-8 assay	[PMID: 29670692]
HT-29	IC₅₀	62.96 μM Compound: Epacadostat	Cytotoxicity against human HT-29 cells assessed as reduction in cell viability by CCK8 assay Cytotoxicity against human HT-29 cells assessed as reduction in cell viability by CCK8 assay	[PMID: 34854662]
Lewis lung carcinoma cell line	IC₅₀	>100 μM Compound: 2; INCB024360	Antiproliferative activity against mouse LLC cells after 48 hrs by CCK-8 assay Antiproliferative activity against mouse LLC cells after 48 hrs by CCK-8 assay	[PMID: 29670692]
MCF7	IC₅₀	>50 μM Compound: Epacadostat	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 34147748]
SW480	IC₅₀	>50 μM Compound: Epacadostat	Cytotoxicity against human SW480 cells measured after 48 hrs by MTT assay Cytotoxicity against human SW480 cells measured after 48 hrs by MTT assay	[PMID: 37060754]
THP-1	IC₅₀	5.6 nM Compound: INCB024360	Inhibition of IDO1 in IFN-gamma/LPS stimulated human THP-1 cells assessed as reduction in kynurenine production after 24 hrs Inhibition of IDO1 in IFN-gamma/LPS stimulated human THP-1 cells assessed as reduction in kynurenine production after 24 hrs	[PMID: 30858027]
U-87MG ATCC	IC₅₀	>50 μM Compound: Epacadostat	Cytotoxicity against human U87 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Cytotoxicity against human U87 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 34147748]
U-87MG ATCC	IC₅₀	0.26 μM Compound: INCB024360	Inhibition of TDO in human U87 MG cells using L-Trp as substrate after 8 hrs Inhibition of TDO in human U87 MG cells using L-Trp as substrate after 8 hrs	[PMID: 30321802]

体外実験

In cellular assays, Epacadostat (INCB 024360) selectively inhibits human IDO1 with IC₅₀ values of approximately 10 nM, demonstrating little activity against other related enzymes such as IDO2 or tryptophan 2,3-dioxygenase (TDO). Epacadostat (INCB 024360) also exhibits significant activity toward mouse IDO1, with an IC₅₀ value of 52.4 nM±15.7 nM, in a similar assay using mouse IDO1-transfected HEK293/MSR cells^[1].

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

体内実験

Female Balb/c mice bearing CT26 tumors are treated orally twice daily for 12 d with Epacadostat at 100 mg/kg. Epacadostat (INCB 024360) suppresses kynurenine equivalently in plasma, tumors, and lymph nodes. In na ve C57BL/6 mice, 50 mg/kg Epacadostat (INCB 024360) decreases plasma kynurenine levels within 1 hour and those levels stay at least 50% suppressed through the 8-hour time course^[2].

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

臨床実験

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

化学情報

CAS 番号 1204669-58-8
性状 Solid
分子量 438.23
分子式 C₁₁H₁₃BrFN₇O₄S
Color White to gray
SMILES

BrC1=C(F)C=CC(N/C(C2=NON=C2NCCNS(N)(=O)=O)=N\O)=C1
別名

INCB 024360
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (28)

All Cell Proliferation/Viability AssayIFCell Imaging/StainingWBFlow CytometryIHC

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Journal Impact Factor

Cancer Discov

Synthetic Essentiality of Tryptophan 2,3-Dioxygenase 2 in APC-Mutated Colorectal Cancer. [Abstract]

2022 Jul 6;12(7):1702-1717. PMID: 35537038
Cancer Commun (Lond)

Interactions of Indoleamine 2,3-dioxygenase-expressing LAMP3+ dendritic cells with CD4+ regulatory T cells and CD8+ exhausted T cells: synergistically remodeling of the immunosuppressive microenvironment in cervical cancer and therapeutic implications. [Abstract]

2023 Nov;43(11):1207-1228. PMID: 37794698
Nat Cell Biol

Peritumoural adipose tissue promotes ferroptosis resistance by 3-hydroxykynurenine-mediated suppression of ferritinophagy. [Abstract]

2026 Apr;28(4):783-796. PMID: 41813885
Cell Host Microbe

Microbiota-induced alteration of kynurenine metabolism in macrophages drives formation of creeping fat in Crohn's disease. [Abstract]

2024 Nov 13;32(11):1927-1943.e9. PMID: 39541945
J Nanobiotechnology

HDACi combination therapy with IDO1i remodels the tumor microenvironment and boosts antitumor efficacy in colorectal cancer with microsatellite stability. [Abstract]

2024 Dec 16;22(1):753. PMID: 39676171

Epacadostat purchased from MedChemExpress. Usage Cited in: J Nanobiotechnology. 2024 Dec 16;22(1):753. [Abstract]

Epacadostat (IDO1i; 25-150 nM; 48 h). Cytotoxicity of NP-I, NP-P, and NP-I/P in vitro.
J Immunother Cancer

Neovascular pruning by IDO1 inhibitors can potentiate immunogenic cytotoxicity of ischemia-targeted agents to synergistically enhance anti-PD-1 responsiveness. [Abstract]

2025 May 30;13(5):e011398. PMID: 40447318

Epacadostat purchased from MedChemExpress. Usage Cited in: J Immunother Cancer. 2025 May 30;13(5):e011398. [Abstract]

Epacadostat (60 mg/kg; p.o.). Representative confocal images of immunofluorescence staining for blood vessels (α-CAV1; Cy3, red), hypoxia (α-Hypoxyprobe; FITC, green), and nuclei (DAPI, blue) in 4T1 lung metastases from WT mice prior to and following epacadostat administration over 72 hours.
Cell Rep Med

An adverse tumor-protective effect of IDO1 inhibition. [Abstract]

2023 Feb 21;4(2):100941. PMID: 36812891

Epacadostat purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2023 Feb 21;4(2):100941. [Abstract]

Cell lines were treated with IFNγ (2.5, 5, or 10 ng/mL) and/or Epacadostat (2 μM), fixed and stained with crystal violet after 6 days.

Epacadostat purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2023 Feb 21;4(2):100941. [Abstract]

Indicated cell lines were treated with IFNγ or with Epacadostat (2 μM) + 5 or 20 ng/mL IFNγ for 72 h and harvested for immunoblotting with the indicated antibodies, all in parallel. Vinculin served as a loading control.
Int J Biol Sci

The IFN-γ-IDO1-kynureine pathway-induced autophagy in cervical cancer cell promotes phagocytosis of macrophage. [Abstract]

2021 Jan 1;17(1):339-352. PMID: 33390854
Br J Pharmacol

LW106, a novel indoleamine 2,3-dioxygenase 1 inhibitor, suppresses tumour progression by limiting stroma-immune crosstalk and cancer stem cell enrichment in tumour micro-environment. [Abstract]

2018 Jul;175(14):3034-3049. PMID: 29722898

Epacadostat purchased from MedChemExpress. Usage Cited in: Br J Pharmacol. 2018 Jul;175(14):3034-3049. [Abstract]

Epacadostat (80 mg/kg; ip). Representative dot plots of CD8⁺ effector T cells of total CD45⁺ cells for vehicle‐, LW106‐ and Epacadostat‐treated mice.

Epacadostat purchased from MedChemExpress. Usage Cited in: Br J Pharmacol. 2018 Jul;175(14):3034-3049. [Abstract]

Epacadostat (80 mg/kg; ip). Representative immunohistochemical images of Ki67‐, phospho‐histone H3‐ and cleaved caspase 3‐positive cells for tumours of indicated mice.
Cell Chem Biol

DELs enable the development of BRET probes for target engagement studies in cells. [Abstract]

2023 Aug 17;30(8):987-998.e24. PMID: 37490918
OncoImmunology

Tumor endothelial cell up-regulation of IDO1 is an immunosuppressive feed-back mechanism that reduces the response to CD40-stimulating immunotherapy. [Abstract]

2020 Mar 9;9(1):1730538. PMID: 32231867
Eur J Med Chem

Discovery of novel hydroxyamidine based indoleamine 2,3-dioxygenase 1 (IDO1) and thioredoxin reductase 1 (TrxR1) dual inhibitors. [Abstract]

2023 Jan 5;245(Pt 1):114860. PMID: 36370550
Bioorg Chem

Design, synthesis, and biological evaluation of a novel indoleamine 2,3-dioxigenase 1 (IDO1) and thioredoxin reductase (TrxR) dual inhibitor. [Abstract]

2020 Dec:105:104401. PMID: 33113415
J Chromatogr A

On-line screening of indoleamine 2,3-dioxygenase 1 inhibitors by partial filling capillary electrophoresis combined with rapid polarity switching. [Abstract]

2021 Aug 16:1651:462305. PMID: 34147833
Sci Rep

Exhaustion of CD4+ T-cells mediated by the Kynurenine Pathway in Melanoma. [Abstract]

2019 Aug 21;9(1):12150. PMID: 31434983
Sci Rep

Endothelial indoleamine 2,3-dioxygenase-1 regulates the placental vascular tone and is deficient in intrauterine growth restriction and pre-eclampsia. [Abstract]

2018 Apr 3;8(1):5488. PMID: 29615752
J Hepatocell Carcinoma

Low Indoleamine 2,3-Dioxygenase 1 Expression Enhances Dendritic Cells Response to Tumor Cells Against Hepatocellular Carcinoma. [Abstract]

2025 Sep 20:12:2149-2167. PMID: 41000276
Toxicol Appl Pharmacol

Indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors activate the aryl hydrocarbon receptor. [Abstract]

2017 May 15:323:74-80. PMID: 28336214
Bioorg Med Chem

Parallel discovery of selective and dual inhibitors of tryptophan dioxygenases IDO1 and TDO2 with a newly-modified enzymatic assay. [Abstract]

2021 Jun 1:39:116160. PMID: 33901770
Toxicol Lett

Aristolochic acid I promotes renal tubulointerstitial fibrosis by up-regulating expression of indoleamine 2,3-dioxygenase-1 (IDO1). [Abstract]

2024 Dec:402:44-55. PMID: 39547317
PLoS One

Inhibition of immune checkpoints PD-1, CTLA-4, and IDO1 coordinately induces immune-mediated liver injury in mice. [Abstract]

2019 May 21;14(5):e0217276. PMID: 31112568
FEBS Open Bio

Indoleamine 2,3-dioxygenase 1 inhibition reverses cancer-associated fibroblast-mediated immunosuppression in high-grade serous ovarian cancer. [Abstract]

2025 Oct 13. PMID: 41078340
bioRxiv

Antigenic cancer persister cells survive direct T cell attack. [Abstract]

2025 Mar 17:2025.03.14.643359. PMID: 40166148
Preprints

2025 Feb 03.
Res Sq

2024 Nov 03.
Res Sq

2024 Nov 25.
The University of New South Wales

2023 Mar.
Methods Mol Biol

Methods for High-throughput Drug Combination Screening and Synergy Scoring. [Abstract]

2018:1711:351-398. PMID: 29344898

溶剤 & 溶解度

体外:

DMSO : 100 mg/mL (228.19 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2819 mL

11.4095 mL

22.8191 mL

5 mM

0.4564 mL

2.2819 mL

4.5638 mL

10 mM

0.2282 mL

1.1410 mL

2.2819 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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濃度濃度

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希釈計算機

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濃度 _(終了) 濃度 _(終了)

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体内:

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

Stock Solution Working Solution

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: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: ≥ 2.62 mg/mL (5.98 mM); Clear solution

Protocol 2

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.62 mg/mL (5.98 mM); Clear solution

Protocol 3

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.70 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.

Protocol 4

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.70 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.

Protocol 5

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.70 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.

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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

プロトコル

Cell Assay^[1]

To determine Epacadostat activity against IDO in recombinant cells, HEK293/MSR cells are transiently transfected with full-length human or mouse IDO1, or mouse IDO2 cDNA, with Transit-293 transfection reagent or Lipofectamine 2000 reagents. Epacadostat (INCB 024360) at different concentrations is added to the recovered transfected cells seeded at 2×10⁴ cells per well in a 96-well plate (200 μL/well). The cells are incubated for 2 days, and kyn in the supernatants is measured as described in the HeLa cell assay. The tryptophan 2,3-dioxygenase (TDO) assay is performed similarly with HEK293/MSR cells transfected with a human TDO expression vector^[1].

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

Animal Administration^[2]

Mice^[2]
The female C57BL/6 mice are dosed orally with 50 mg/kg Epacadostat. C57BL/6 wild-type or Ido1^-/--deficient mice are administered a single oral dose of Epacadostat (INCB 024360), at which point food is removed from the cages until after the 8-h time point. At various time points after dosing, mice are euthanized and blood is collected by cardiac puncture. Plasma is analyzed for the presence of Epacadostat (INCB 024360), tryptophan, and kynurenine according to the methods below.

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

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (285 KB)
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COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Liu X, et al. Selective inhibition of IDO1 effectively regulates mediators of antitumor immunity. Blood. 2010 Apr 29;115(17):3520-30. [Content Brief]

[2]. Koblish HK, et al. Hydroxyamidine inhibitors of indoleamine-2,3-dioxygenase potently suppress systemic tryptophan catabolism and the growth of IDO-expressing tumors. Mol Cancer Ther. 2010 Feb;9(2):489-98. [Content Brief]

[3]. Fu R, et al. LW106, a novel indoleamine 2,3-dioxygenase 1 inhibitor, suppresses tumour progression by limiting stroma-immune crosstalk and cancer stem cell enrichment in tumour micro-environment. Br J Pharmacol. 2018 Jul;175(14):3034-3049. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2819 mL	11.4095 mL	22.8191 mL	57.0477 mL
	5 mM	0.4564 mL	2.2819 mL	4.5638 mL	11.4095 mL
	10 mM	0.2282 mL	1.1410 mL	2.2819 mL	5.7048 mL
	15 mM	0.1521 mL	0.7606 mL	1.5213 mL	3.8032 mL
	20 mM	0.1141 mL	0.5705 mL	1.1410 mL	2.8524 mL
	25 mM	0.0913 mL	0.4564 mL	0.9128 mL	2.2819 mL
	30 mM	0.0761 mL	0.3803 mL	0.7606 mL	1.9016 mL
	40 mM	0.0570 mL	0.2852 mL	0.5705 mL	1.4262 mL
	50 mM	0.0456 mL	0.2282 mL	0.4564 mL	1.1410 mL
	60 mM	0.0380 mL	0.1902 mL	0.3803 mL	0.9508 mL
	80 mM	0.0285 mL	0.1426 mL	0.2852 mL	0.7131 mL
	100 mM	0.0228 mL	0.1141 mL	0.2282 mL	0.5705 mL

Keywords

Epacadostat

28 Cited Publications

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Epacadostat

Immunology/Inflammation Compound Library

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MedChemExpress（MCE）の使用を引用している文献 Epacadostat

Indoleamine 2,3-Dioxygenase (IDO) アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (28)

溶剤 & 溶解度

プロトコル

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

Epacadostat

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Small Molecule Immuno-Oncology Compound Library

Drug Repurposing Compound Library

Anti-COVID-19 Compound Library

Anti-Pancreatic Cancer Compound Library

Targeted Diversity Library

Rare Diseases Drug Library

Anti-Prostate Cancer Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

MedChemExpress（MCE）の使用を引用している文献 Epacadostat

Indoleamine 2,3-Dioxygenase (IDO) アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (28)

溶剤 & 溶解度

プロトコル

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

Epacadostat 関連分類

HY-15689 関連分類