Epacadostat (INCB024360)

製品コードS7910 バッチS791004

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₁H₁₃BrFN₇O₄S
	分子量	438.23	CAS No.	1204669-58-8
Solubility (25°C)*	体外	DMSO	87 mg/mL (198.52 mM)
		Ethanol	87 mg/mL warmed with 50ºC water bath (198.52 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Epacadostat (INCB024360) is a potent and selective indoleamine 2,3-dioxygenase (IDO1) inhibitor with IC50 of 10 nM and displays high selectivity over other related enzymes such as IDO2 or tryptophan 2,3-dioxygenase (TDO).
in vitro	In IFN-γ–treated human HeLa cells, INCB024360 potently inhibits kynurenine production. INCB024360 also promotes T and natural killer (NK)-cell growth, increases IFN-gamma production, and reduces conversion to regulatory T (T(reg))-like cells. ^[1]
in vivo	INCB024360 (100 mg/kg, p.o.), via IDO1 inhibition, suppresses kyn generation and tumor growth in immunocompetent, but not immunodeficient, mice. ^[1] In mice bearing CT26 colon carcinoma, INCB024360 (100 mg/kg, p.o.) also inhibits the growth of IDO-expressing tumors by reducing kynurenine. ^[2]

製品説明

Epacadostat (INCB024360) is a potent and selective indoleamine 2,3-dioxygenase (IDO1) inhibitor with IC50 of 10 nM and displays high selectivity over other related enzymes such as IDO2 or tryptophan 2,3-dioxygenase (TDO).

in vitro

In IFN-γ–treated human HeLa cells, INCB024360 potently inhibits kynurenine production. INCB024360 also promotes T and natural killer (NK)-cell growth, increases IFN-gamma production, and reduces conversion to regulatory T (T(reg))-like cells. ^[1]

in vivo

INCB024360 (100 mg/kg, p.o.), via IDO1 inhibition, suppresses kyn generation and tumor growth in immunocompetent, but not immunodeficient, mice. ^[1]

In mice bearing CT26 colon carcinoma, INCB024360 (100 mg/kg, p.o.) also inhibits the growth of IDO-expressing tumors by reducing kynurenine. ^[2]

プロトコル(参考用のみ)

キナーゼアッセイ	IDO enzyme assays
キナーゼアッセイ	Human IDO with an N-terminal His tag is expressed in E.coli and purified to homogeneity. IDO catalyzes the oxidative cleavage of the pyrrole ring of the indole nucleus of tryptophan to yield N’-formylkynurenine. The assays are performed at room temperature using 20 nM IDO and 2 mM D-Trp in the presence of 20 mM ascorbate, 3.5 µM methylene blue and 0.2 mg/mL catalase in 50 mM potassium phosphate buffer (pH 6.5). The initial reaction rates are recorded by continuously following the absorbance increase at 321 nm due to the formation of N’-formlylkynurenine.
細胞アッセイ	細胞株	Jurkat cells
	濃度	50 μM
	反応時間	72 h
	実験の流れ	Jurkat cells were incubated with serially diluted epacadostat for 72 h. Their viability was measured and analyzed as percentage of the non-treated control.
動物実験	動物モデル	Female C57BL/6 or Balb/c nu/nu mice bearing PAN02 pancreatic tumors
	投薬量	~100 mg/kg, twice a day
	投与方法	p.o.

参考

カスタマーフィードバック

: Data from [Data independently produced by , , FEBS J, 2016, doi: 10.1111/febs.13966.]

: Data from [Data independently produced by , , Cancer Immunol Immunother, 2018, 67(8):1305-1315]

: Data from [Data independently produced by , , Mol Immunol, 2018, 103:144-155]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Loss of tumor suppressors promotes inflammatory tumor microenvironment and enhances LAG3+T cell mediated immune suppression [ Nat Commun, 2024, 15(1):5873]	PubMed: 38997291
Metabolic landscape of head and neck squamous cell carcinoma informs a novel kynurenine/Siglec-15 axis in immune escape [ Cancer Commun (Lond), 2024, 44(6):670-694]	PubMed: 38734931
Metabolic landscape of head and neck squamous cell carcinoma informs a novel kynurenine/Siglec-15 axis in immune escape [ Cancer Commun (Lond), 2024, 10.1002/cac2.12545]	PubMed: 38734931
Single-cell RNA sequencing highlights the immunosuppression of IDO1+ macrophages in the malignant transformation of oral leukoplakia [ Theranostics, 2024, 14(12):4787-4805]	PubMed: 39239507
Tryptophan deficiency induced by indoleamine 2,3-dioxygenase 1 results in glucose transporter 1-dependent promotion of aerobic glycolysis in pancreatic cancer [ MedComm (2020), 2024, 5(5):e555]	PubMed: 38706741
Epacadostat stabilizes the apo-form of IDO1 and signals a pro-tumorigenic pathway in human ovarian cancer cells [ Front Immunol, 2024, 15:1346686]	PubMed: 38333210
IDO1 Inhibitor RY103 Suppresses Trp-GCN2-Mediated Angiogenesis and Counters Immunosuppression in Glioblastoma [ Pharmaceutics, 2024, 16(7)870]	PubMed: 39065567
Selective inhibition of indoleamine and tryptophan 2,3-dioxygenases: Comparative study on kynurenine pathway in cell lines via LC-MS/MS-based targeted metabolomics [ J Pharm Biomed Anal, 2024, 237:115750]	PubMed: 37804639
Blocking Tryptophan Catabolism Reduces Triple-Negative Breast Cancer Invasive Capacity [ Cancer Res Commun, 2024, 4(10):2699-2713]	PubMed: 39311710
Targeting Tryptophan Catabolism in Ovarian Cancer to Attenuate Macrophage Infiltration and PD-L1 Expression [ Cancer Res Commun, 2024, 4(3):822-833]	PubMed: 38451784

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。